Bortezomib

别名: LDP-341, MLM341, NSC 681239,PS-341, BTZ 中文名称：硼替佐米

此产品请避光密封保存。

目录号：S1013 Purity: 99.97%

Bortezomib是有效的蛋白酶体抑制剂，K_i为0.6 nM。它对肿瘤细胞表现出良好的选择性。Bortezomib可抑制 NF-κB 并诱导 ERK 的磷酸化从而抑制cathepsin B并在卵巢癌和其他固体肿瘤中抑制自噬的催化过程。

Bortezomib Chemical Structure

CAS: 179324-69-7

规格	价格	库存
10mM (1mL in DMSO)	749.39	现货
5mg	571.94	现货
25mg	1613.43	现货
100mg	4316.13	现货
1g	7944.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.97%

99.97

Bortezomib相关产品

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
human PBMC	Function Assay	100 nM	24 h	Induces IL-8 release	25791477
U937	Function Assay	100 nM	6 h	Induces IL-8 expression in LPS-stimulated U937 macrophages	25791477
HH	Migration Assay	100 nM	24 h	Reduces cell migration by 80–91%	25681335
Hut-78	Migration Assay	100 nM	24 h	Reduces cell migration by 80–90%	25681335
HH	Function Assay	100 nM	24 h	downregulates TGF-β1 and IL-12 expression	25681335
H9	Function Assay	100 nM	24 h	Downregulates TGF-β1 and IL-11 expression	25681335
Hut-78	Function Assay	100 nM	24 h	Downregulates TGF-β1 and IL-10 expression	25681335
H1299	Apoptosis Assay	80 nM	24 h	Sensitizes NSCLC cells to MSC-derived iC9-induced apoptosis	25323693
BLM	Autophagy Assay	10 nM	12 h	Induces formation of autophagosomes	23079083
A375	Autophagy Assay	10 nM	12 h	Induces formation of autophagosomes	23079083
BLM	Apoptosis Assay	10 nM	24 h	Induces cell apoptosis	23079083
A375	Apoptosis Assay	10 nM	24 h	Induces cell apoptosis	23079083
RAW 264.7	Growth Inhibition Assay	100 nM	48 h	Reduces cell viability	22427154
SNK-6	Antiviral Assay	1 μM	24 h	Induces lytic infection of EBV	21170988
KAI-3	Antiviral Assay	1 μM	24 h	Induces lytic infection of EBV	21170988
SNT-16	Antiviral Assay	1 μM	24 h	Induces lytic infection of EBV	21170988
SNT-13	Antiviral Assay	1 μM	24 h	Induces lytic infection of EBV	21170988
KHYG-1	Apoptosis Assay	1 μM	6 h	Induces cell apoptosis	21170988
KAI-3	Apoptosis Assay	1 μM	6 h	Induces cell apoptosis	21170988
Jurkat	Apoptosis Assay	1 μM	6 h	Induces cell apoptosis	21170988
SNT-16	Apoptosis Assay	1 μM	6 h	Induces cell apoptosis	21170988
KHYG-1	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
SNK-6	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
KAI-3	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
Jurkat	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
SNT-16	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
SNT-13	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
BJAB	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
LCL-2	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
LCL-1	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
Raji	Growth Inhibition Assay	1 μM	24 h	Reduces cell viability	21170988
BaF/3-p210	Function Assay	6 nM	24 h	Reduces the phosphorylation and the activity of Rb	20305692
BaF/3-p210	Function Assay	6 nM	48 h	Induces a slight G1 cell-cycle arrest	20305692
BaF/3	Function Assay	6 nM	48 h	Induces a great G1 cell-cycle arrest	20305692
TCC-S	Growth Inhibition Assay	100 nM	48 h	IC50=2.8 nM	20305692
BaF/3-p210	Growth Inhibition Assay	100 nM	48 h	IC50=4.7 nM	20305692
BaF/3	Growth Inhibition Assay	100 nM	48 h	IC50=6.2 nM	20305692
RPMI 8226	Function Assay	20 nM	8 h	Induces DNA synthesis	19436050
OPM2	Function Assay	20 nM	8 h	Significantly enhances NF-κB activity	19436050
INA6	Function Assay	20 nM	8 h	Significantly enhances NF-κB activity	19436050
OPM1	Function Assay	20 nM	8 h	Significantly enhances NF-κB activity	19436050
U266	Function Assay	20 nM	8 h	Significantly enhances NF-κB activity	19436050
MM.1S	Function Assay	20 nM	8 h	Significantly enhances NF-κB activity	19436050
RPMI 8226	Function Assay	20 nM	8 h	Significantly enhances NF-κB activity	19436050
CHLA-255	Function Assay	10 nM	24 h	Modestly reduces cells in the G0/G1 phase	17689684
NB-1691	Function Assay	10 nM	24 h	Significantly reduces cells in the G0/G1 phase	17689684
SK-N-AS	Growth Inhibition Assay	1 μM	72 h	Inhibits cell proliferation to 10%	17689684
CHLA-255	Growth Inhibition Assay	1 μM	72 h	Inhibits cell proliferation to 2%	17689684
NB-1691	Growth Inhibition Assay	1 μM	72 h	Inhibits cell proliferation to 5%	17689684
HKe-3	Apoptosis Assay	50 nM	48 h	Induces cell apoptosis	16778179
HCT116	Apoptosis Assay	50 nM	48 h	Induces cell apoptosis	16778179
T29Kt1	Apoptosis Assay	50 nM	48 h	Induces cell apoptosis	16778179
T29	Apoptosis Assay	50 nM	48 h	Induces cell apoptosis	16778179
LNCap-Pro5	Function Assay	1 μM	4 h	Stabilizes p53	14612532
H460	Function Assay	100 nM	24 h	Induces G2-M-phase arrest and tubulin assembly-disassembly	12631620
H322	Growth Inhibition Assay	10 μM	72 h	IC50=620 nM	12631620
H358	Growth Inhibition Assay	10 μM	72 h	IC50=70 nM	12631620
H460	Growth Inhibition Assay	10 μM	72 h	IC50=100 nM	12631620
RPMI8226/LR5	Growth Inhibition Assay	500 ng/ml	48 h	Inhibits cell growth	12631619
U266/dox4	Growth Inhibition Assay	500 ng/ml	48 h	Inhibits cell growth	12631619
U266/LR7	Growth Inhibition Assay	500 ng/ml	48 h	Inhibits cell growth	12631619
WAD-1	Growth Inhibition Assay	500 ng/ml	48 h	Inhibits cell growth	12631619
ARH77	Growth Inhibition Assay	500 ng/ml	48 h	Inhibits cell growth	12631619
U266	Growth Inhibition Assay	500 ng/ml	48 h	Inhibits cell growth	12631619
H460	Function Assay	10 μM	24 h	Induces Bcl-2 phosphorylation and cleavage correlated with G2-M phase arrest	12492117
UM-SCC-11B	Growth Inhibition Assay	100 nM	72 h	Inhibits cell viability	11350913
UM-SCC-9	Growth Inhibition Assay	100 nM	72 h	Inhibits cell viability	11350913
B7E3	Growth Inhibition Assay	100 nM	72 h	Inhibits cell viability	11350913
B4B8	Growth Inhibition Assay	100 nM	72 h	Inhibits cell viability	11350913
PAM-LY2	Growth Inhibition Assay	100 nM	72 h	Inhibits cell viability	11350913
PAM 212	Growth Inhibition Assay	100 nM	72 h	Inhibits cell viability	11350913
PAM-LY2	Function Assay	100 nM	12 h	Inhibits NF-κB activation	11350913
Hs Sultan	Growth Inhibition Assay	100 nM	48 h	IC50=20 nM	11306489
IM-9	Growth Inhibition Assay	100 nM	48 h	IC50=6 nM	11306489
U266	Growth Inhibition Assay	100 nM	48 h	IC50=3 nM	11306489
LR5	Growth Inhibition Assay	100 nM	48 h	IC50=20 nM	11306489
MR20	Growth Inhibition Assay	100 nM	48 h	IC50=20 nM	11306489
Dox40	Growth Inhibition Assay	100 nM	48 h	IC50=40 nM	11306489
RPMI8226	Growth Inhibition Assay	100 nM	48 h	IC50=30 nM	11306489
OVCA 429	Function Assay	300 nM	48 h	Disrupts intact multicellular tumor spheroids	10999766
MCF-7	Cytotoxic Assay	50 μM	48 h	Kills cells by more than 99%	10499643
HeLa	Function assay	5 nM	8 hrs	Inhibition of proteasome activity in human HeLa cells assessed as induction of ubiquitinG76V-FL reporter level at 5 nM after 8 hrs by luciferase assay	21186794
HeLa	Function assay	1 uM	8 hrs	Inhibition of proteasome activity in human HeLa cells assessed as induction of ubiquitinG76V-FL reporter level at 1 uM after 8 hrs by luciferase assay	21186794
LN229	Function assay	100 nM	1 hr	Inhibition of HIF1alpha expression in human LN229 cells assessed as reduction of HIF-1alpha accumulation at 100 nM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by Western blotting	21831638
LN229	Function assay	20 uM	1 hr	Inhibition of hypoxia-induced HIF1alpha accumulation in human LN229 cells at 20 uM after 1 hr preincubation measured after 24 hrs by Western blot analysis	22032632
U1	Function assay	10 uM	24 hr	Inhibition of NF-kappaB-mediated viral replication in Homo sapiens (human) U1 cells infected with X4 tropic HIV1 NL4-3 at 10 uM after 24 hr by RT-PCR analysis in presence of TNF-alpha	23290051
Calu6	Function assay	10 uM	18 hrs	Inhibition of His-tagged Frataxin (unknown origin)/Ubiquitin interaction expressed in human Calu6 cells assessed as increase in frataxin (1-210) precursor level at 10 uM after 18 hrs by Western blotting analysis	23506486
HEK293	Cytotoxicity assay	0.0001 uM to 100 uM	48 hrs	Cytotoxicity against human HEK293 cells expressing murine FAP at 0.0001 uM to 100 uM after 48 hrs by CellTiter-Blue assay	23594271
A549	Function assay	0.025 to 0.5 uM	24 hrs	Induction of cell death in human A549 cells assessed as accumulation of poly-ubiquitinated proteins at 0.025 to 0.5 uM after 24 hrs by immunoblot assay	25639862
A549	Function assay	0.025 to 0.5 uM	24 hrs	Induction of cell death in human A549 cells assessed as stabilization of p53 at 0.025 to 0.5 uM after 24 hrs by immunoblot assay	25639862
A549	Function assay	0.025 to 0.1 uM	24 hrs	Induction of cell death in human A549 cells assessed as accumulation of Noxa at 0.025 to 0.1 uM after 24 hrs by immunoblot assay	25639862
MCF7	Function assay	35 nM	4 hrs	Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis	27994734
MDA-MB-468	Function assay	35 nM	4 hrs	Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis	27994734
SK-N-SH	Cytotoxicity assay	0.1 to 1 uM	24 hrs	Cytotoxicity against human SK-N-SH cells assessed as reduction in cell viability at 0.1 to 1 uM after 24 hrs by MTT assay	29269255
MYCN2	Cytotoxicity assay	0.1 to 1 uM	24 hrs	Cytotoxicity against human MYCN2 cells assessed as reduction in cell viability at 0.1 to 1 uM after 24 hrs by MTT assay	29269255
U266	Apoptosis assay	2.5 nM	24 hrs	Induction of apoptosis in human U266 cells at 2.5 nM after 24 hrs by Annexin V/propidium iodide staining based flow cytometry	29304284
RPMI8226	Apoptosis assay	2.5 nM	24 hrs	Induction of apoptosis in human RPMI8226 cells at 2.5 nM after 24 hrs by Annexin V/propidium iodide staining based flow cytometry	29304284
NCI-H929	Apoptosis assay	2.5 nM	24 hrs	Induction of apoptosis in human NCI-H929 cells at 2.5 nM after 24 hrs by Annexin V/propidium iodide staining based flow cytometry	29304284
HL60	Function assay	1 to 100 nM	24 hrs	Inhibition of proteasome in human HL60 cells assessed as increase in cleaved PARP expression at 1 to 100 nM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	1 to 100 nM	24 hrs	Inhibition of proteasome in imatinib-resistant human SUP-B15 cells assessed as increase in cleaved PARP expression at 1 to 100 nM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	1 to 100 nM	24 hrs	Inhibition of proteasome in human SEM cells assessed as increase in cleaved PARP expression at 1 to 100 nM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	10 nM	18 hrs	Inhibition of proteasome in human SEM cells assessed as increase in aggresome accumulation at 10 nM after 18 hrs by by FACS analysis	30365892
SEM	Function assay	10 nM	18 hrs	Inhibition of proteasome in human SEM cells assessed as increase in aggresome accumulation at 10 nM after 18 hrs by fluorescence microscopic method	30365892
HL60	Function assay	100 nM		Inhibition of chymotrypsin-like activity of proteasome in human HL60 cells at 100 nM	19655762
AMO1	Antitumor assay	1 mg/kg		Antitumor activity against human AMO1 cells xenografted in nude SCID beige mouse assessed as tumor growth inhibition at 1 mg/kg, iv administered twice per week	26565666
MDA-MB-231	Function assay	1 uM		Inhibition of trypsin like activity of 26S proteasome derived from human MDA-MB-231 cells at 1 uM	28291344
MDA-MB-231	Function assay	1 uM		Inhibition of caspase like activity of 26S proteasome derived from human MDA-MB-231 cells at 1 uM	28291344
MDA-MB-231	Function assay	1 uM		Inhibition of chymotrypsin like activity of 26S proteasome derived from human MDA-MB-231 cells at 1 uM	28291344
FSCLL	Cytotoxicity assay		24 hrs	CC50 = 0.004 μM	21634429
HEK293	Cytotoxicity assay		24 hrs	CC50 = 0.347 μM	21634429
Glioma (HF2303)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
Glioma (HF2476)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
Glioma (HF2876)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
Glioma (HF2885)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
Glioma (HF3013)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
Glioma (HF2381)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
Glioma (HF2790)	Cytotoxicity assay		72 hrs	EC50 = 0.0007 μM	26288699
HepG2	Cytotoxicity assay		48 hrs	EC50 = 0.01 μM	29800827
HL60	Function assay		10 mins	ED50 = 0.0025 μM	19422206
HL60	Function assay		10 mins	ED50 = 0.0025 μM	21973101
CEM	Antiproliferative assay		72 hrs	GI50 = 0.001 μM	28441582
U266	Antiproliferative assay		72 hrs	GI50 = 0.001 μM	28441582
K562	Antiproliferative assay		72 hrs	GI50 = 0.007 μM	28441582
DLD1	Function assay		6 hrs	IC50 = 0.0002 μM	22206869
DLD1	Function assay		6 hrs	IC50 = 0.0009 μM	22206869
HCT116	Cytotoxicity assay		72 hrs	IC50 = 0.001 μM	28634039
HCT116	Antiproliferative assay		72 hrs	IC50 = 0.0014 μM	27769033
HepG2	Antiproliferative assay		72 hrs	IC50 = 0.00161 μM	27769033
SKOV3	Antiproliferative assay		72 hrs	IC50 = 0.00162 μM	27769033
DOGUM	Cytotoxicity assay		72 hrs	IC50 = 0.002 μM	23031590
U266	Cytotoxicity assay		72 hrs	IC50 = 0.00245 μM	19537716
A549	Antiproliferative assay		72 hrs	IC50 = 0.0025 μM	28182990
HL60	Antiproliferative assay		72 hrs	IC50 = 0.0032 μM	28182990
RPMI18226	Cytotoxicity assay		72 hrs	IC50 = 0.0035 μM	21077681
HL60	Cytotoxicity assay		72 hrs	IC50 = 0.0035 μM	21077681
RPMI8226	Cytotoxicity assay		72 hrs	IC50 = 0.00388 μM	26965867
HL60	Function assay		2 hrs	IC50 = 0.004 μM	27769033
U266	Function assay		1 hr	IC50 = 0.004 μM	28441582
HL60	Function assay		2 hrs	IC50 = 0.004 μM	28634039
SEM	Function assay		2 hrs	IC50 = 0.00443 μM	30365892
HL60	Cytotoxicity assay		72 hrs	IC50 = 0.0055 μM	19537716
U266	Cytotoxicity assay		72 hrs	IC50 = 0.00573 μM	26965867
MGC803	Antiproliferative assay		72 hrs	IC50 = 0.005782 μM	27769033
GUMBUS	Cytotoxicity assay		72 hrs	IC50 = 0.006 μM	23031590
ARH77	Cytotoxicity assay		72 hrs	IC50 = 0.00607 μM	26965867
SW480	Cytotoxicity assay		72 hrs	IC50 = 0.0061 μM	20158184
MDA-MB-231	Antiproliferative assay		72 hrs	IC50 = 0.0065 μM	28182990
HL60	Function assay		2 hrs	IC50 = 0.00667 μM	30365892
A549	Cytotoxicity assay		72 hrs	IC50 = 0.0067 μM	20158184
RPMI8226	Antiproliferative assay		72 hrs	IC50 = 0.0067 μM	28182990
5TGM1	Cytotoxicity assay		48 to 72 hrs	IC50 = 0.00678 μM	24119559
HL60	Cytotoxicity assay		72 hrs	IC50 = 0.0069 μM	19747832
PC3	Cytotoxicity assay		72 hrs	IC50 = 0.007 μM	20158184
DOGUM	Cytotoxicity assay		72 hrs	IC50 = 0.007 μM	23031590
HL60	Cytotoxicity assay		72 hrs	IC50 = 0.0071 μM	20158184
MKN45	Antiproliferative assay		72 hrs	IC50 = 0.00715 μM	27769033
HepG2	Cytotoxicity assay		72 hrs	IC50 = 0.0075 μM	20158184
HL60	Antiproliferative assay		72 hrs	IC50 = 0.0076 μM	27769033
RPMI8226	Cytotoxic activity against human		72 hrs	IC50 = 0.00796 μM	24767818
HL60	Cytotoxicity assay		72 hrs	IC50 = 0.008 μM	28634039
MGC803	Cytotoxicity assay		72 hrs	IC50 = 0.008 μM	28634039
SKOV3/TR	Function assay		4 days	IC50 = 0.008 μM	29767973
PC3	Cytotoxicity assay		72 hrs	IC50 = 0.0083 μM	21077681
U266	Cytotoxicity assay		72 hrs	IC50 = 0.0088 μM	20158184
RPMI8226	Cytotoxicity assay		48 to 72 hrs	IC50 = 0.0095 μM	24119559
ARH77	Cytotoxicity assay		72 hrs	IC50 = 0.00957 μM	29934218
HEK293	Function assay		3 hrs	IC50 = 0.01 μM	20875739
HCT116	Cytotoxicity assay		72 hrs	IC50 = 0.01 μM	23547757
NCI-H929	Cytotoxicity assay		72 hrs	IC50 = 0.01085 μM	24767818
CCRF-CEM	Antiproliferative assay		72 hrs	IC50 = 0.011 μM	26231162
RPMI8226	Cytotoxicity assay		72 hrs	IC50 = 0.0112 μM	29934218
U266B1	Cytotoxicity assay		72 hrs	IC50 = 0.01163 μM	29934218
BxPC3	Cytotoxicity assay		72 hrs	IC50 = 0.0118 μM	19747832
293T	Antiproliferative assay		72 hrs	IC50 = 0.012 μM	28191850
U266	Cytotoxicity assay		72 hrs	IC50 = 0.0122 μM	19747832
SW480	Cytotoxicity assay		72 hrs	IC50 = 0.0123 μM	21077681
SKOV3	Cytotoxicity assay		4 days	IC50 = 0.0129 μM	29767973
A549	Cytotoxicity assay		72 hrs	IC50 = 0.0139 μM	21077681
HEK293	Function assay		30 mins	IC50 = 0.014 μM	21044847
RPMI8266	Antiproliferative assay		72 hrs	IC50 = 0.0144 μM	26231162
BxPC3	Cytotoxicity assay		72 hrs	IC50 = 0.0162 μM	20158184
MDA-MB-231	Antiproliferative assay		72 hrs	IC50 = 0.01665 μM	27769033
TOV21G	Antiproliferative assay		72 hrs	IC50 = 0.0167 μM	26231162
MDA-MB-231	Cytotoxicity assay		72 hrs	IC50 = 0.017 μM	28634039
BxPC3	Cytotoxicity assay		72 hrs	IC50 = 0.0194 μM	21077681
HeLa	Growth inhibition assay		72 hrs	IC50 = 0.02 μM	19428245
RKO	Antiproliferative assay		72 hrs	IC50 = 0.0208 μM	26231162
MCF7	Antiproliferative assay		3 days	IC50 = 0.025 μM	28557430
Bel7404	Antiproliferative assay		72 hrs	IC50 = 0.02504 μM	27769033
HepG2	Cytotoxicity assay		72 hrs	IC50 = 0.0252 μM	21077681
HEK293	Function assay		24 hrs	IC50 = 0.027 μM	21634429
HCT116	Antiproliferative assay		72 hrs	IC50 = 0.027 μM	26231162
SUP-B15	Function assay		2 hrs	IC50 = 0.02809 μM	30365892
A431	Antiproliferative assay		72 hrs	IC50 = 0.0282 μM	26231162
A2780	Antiproliferative assay		72 hrs	IC50 = 0.0289 μM	28182990
HL60	Function assay		2 hrs	IC50 = 0.03 μM	27769033
HL60	Function assay		2 hrs	IC50 = 0.03 μM	28634039
HEK293	Function assay		6 hrs	IC50 = 0.03 μM	28919340
WM266.4	Cytotoxicity assay		72 hrs	IC50 = 0.035 μM	22206869
GUMBUS	Cytotoxicity assay		72 hrs	IC50 = 0.035 μM	23031590
HepG2	Cytotoxicity assay		72 hrs	IC50 = 0.0375 μM	19537716
95-D	Cytotoxicity assay		72 hrs	IC50 = 0.038 μM	28634039
95-D	Antiproliferative assay		72 hrs	IC50 = 0.03818 μM	27769033
SW480	Cytotoxicity assay		72 hrs	IC50 = 0.05 μM	19537716
KB	Cytotoxicity assay		72 hrs	IC50 = 0.0595 μM	19537716
SKOV3	Cytotoxicity assay		72 hrs	IC50 = 0.0668 μM	21077681
SW1990	Antiproliferative assay		72 hrs	IC50 = 0.07906 μM	27769033
HeLa	Cytotoxicity assay		72 hrs	IC50 = 0.092 μM	19537716
A549	Antiproliferative assay		72 hrs	IC50 = 0.092 μM	28191850
H460	Cytotoxicity assay		72 hrs	IC50 = 0.115 μM	19537716
SKOV3	Cytotoxicity assay		72 hrs	IC50 = 0.13 μM	19537716
SKOV3	Cytotoxicity assay		72 hrs	IC50 = 0.151 μM	20158184
A549	Cytotoxicity assay		72 hrs	IC50 = 0.255 μM	19537716
HL60	Function assay		2 hrs	IC50 = 0.44 μM	27769033
HL60	Function assay		2 hrs	IC50 = 0.44 μM	28634039
H460	Cytotoxicity assay		72 hrs	IC50 = 0.78 μM	20158184
BGC823	Cytotoxicity assay		72 hrs	IC50 = 0.88 μM	19537716
MCF7	Antiproliferative assay		72 hrs	IC50 = 18.37 μM	29426629
A549	Antiproliferative assay		72 hrs	IC50 = 2.13573 μM	27769033
A549	Cytotoxicity assay		72 hrs	IC50 = 2.14 μM	28634039
BGC823	Cytotoxicity assay		72 hrs	IC50 = 2.89 μM	19747832
MDA-MB-231	Antiproliferative assay		72 hrs	IC50 = 3.125 μM	29426629
BCG823	Cytotoxicity assay		72 hrs	IC50 = 3.29 μM	20158184
A549	Antiproliferative assay		72 hrs	IC50 = 9.318 μM	29426629
Calu6	Cytotoxicity assay		72 hrs	LC50 = 0.0061 μM	20875739
HEK293T	Antiproliferative assay		48 hrs	LC50 = 0.016 μM	29843100
LO2	Antiproliferative assay		48 hrs	LC50 = 0.398 μM	29843100
NCI-H929	Cytotoxicity assay		48 hrs	LD50 = 0.0066 μM	27994734
U266	Cytotoxicity assay		48 hrs	LD50 = 0.018 μM	27994734
LCL	Cytotoxicity assay		48 hrs	LD50 = 0.02 μM	27994734
MDA-MB-468	Cytotoxicity assay		48 hrs	LD50 = 0.037 μM	27994734
RD-ES	Cytotoxicity assay		48 hrs	LD50 = 0.04 μM	27994734
WE68	Cytotoxicity assay		48 hrs	LD50 = 0.1 μM	27994734
IMR90	Cytotoxicity assay		48 hrs	LD50 = 0.13 μM	27994734
KGN	Cytotoxicity assay		48 hrs	LD50 = 0.18 μM	27994734
HNDF	Cytotoxicity assay		48 hrs	LD50 = 0.48 μM	27994734
MCF10A	Cytotoxicity assay		48 hrs	LD50 = 1.5 μM	27994734
SKOV3	Cytotoxicity assay		48 hrs	LD50 = 1.6 μM	27994734
MCF7	Cytotoxicity assay		48 hrs	LD50 = 9.8 μM	27994734
HCT116	Cell cycle assay		24 hrs	Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase after 24 hrs by propidium iodide staining-based flow cytometric analysis	23547757
K-562	Growth Inhibition Assay			IC50=4.12 nM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=4.13 nM	SANGER
OMC-1	Growth Inhibition Assay			IC50=4.18 nM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=4.22 nM	SANGER
TE-12	Growth Inhibition Assay			IC50=4.25 nM	SANGER
NOMO-1	Growth Inhibition Assay			IC50=4.33 nM	SANGER
Raji	Growth Inhibition Assay			IC50=4.46 nM	SANGER
NALM-6	Growth Inhibition Assay			IC50=4.49 nM	SANGER
HL-60	Growth Inhibition Assay			IC50=4.67 nM	SANGER
IST-SL1	Growth Inhibition Assay			IC50=4.68 nM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=4.86 nM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=4.91 nM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=5 nM	SANGER
SBC-1	Growth Inhibition Assay			IC50=5.01 nM	SANGER
CHP-126	Growth Inhibition Assay			IC50=5.06 nM	SANGER
LU-139	Growth Inhibition Assay			IC50=5.13 nM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=5.17 nM	SANGER
SW962	Growth Inhibition Assay			IC50=5.21 nM	SANGER
EW-1	Growth Inhibition Assay			IC50=5.31 nM	SANGER
NCI-H1417	Growth Inhibition Assay			IC50=5.51 nM	SANGER
LU-65	Growth Inhibition Assay			IC50=5.84 nM	SANGER
D-502MG	Growth Inhibition Assay			IC50=6.37 nM	SANGER
BC-3	Growth Inhibition Assay			IC50=6.61 nM	SANGER
GDM-1	Growth Inhibition Assay			IC50=6.77 nM	SANGER
NCI-H2196	Growth Inhibition Assay			IC50=6.8 nM	SANGER
NB1	Growth Inhibition Assay			IC50=6.88 nM	SANGER
NCI-H345	Growth Inhibition Assay			IC50=7.2 nM	SANGER
SU-DHL-1	Growth Inhibition Assay			IC50=7.24 nM	SANGER
JVM-2	Growth Inhibition Assay			IC50=7.28 nM	SANGER
LU-134-A	Growth Inhibition Assay			IC50=7.39 nM	SANGER
NCI-H1694	Growth Inhibition Assay			IC50=7.58 nM	SANGER
NCI-SNU-16	Growth Inhibition Assay			IC50=7.65 nM	SANGER
L-363	Growth Inhibition Assay			IC50=7.7 nM	SANGER
KG-1	Growth Inhibition Assay			IC50=7.94 nM	SANGER
MN-60	Growth Inhibition Assay			IC50=8.14 nM	SANGER
NB6	Growth Inhibition Assay			IC50=8.48 nM	SANGER
MLMA	Growth Inhibition Assay			IC50=8.85 nM	SANGER
ATN-1	Growth Inhibition Assay			IC50=8.89 nM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=9.01 nM	SANGER
DMS-114	Growth Inhibition Assay			IC50=9.62 nM	SANGER
CTB-1	Growth Inhibition Assay			IC50=9.67 nM	SANGER
NCI-H2081	Growth Inhibition Assay			IC50=10.09 nM	SANGER
ES5	Growth Inhibition Assay			IC50=10.38 nM	SANGER
HCC1599	Growth Inhibition Assay			IC50=11.91 nM	SANGER
NCI-H23	Growth Inhibition Assay			IC50=12.12 nM	SANGER
NCI-H1581	Growth Inhibition Assay			IC50=12.28 nM	SANGER
JVM-3	Growth Inhibition Assay			IC50=12.99 nM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=13.19 nM	SANGER
NB7	Growth Inhibition Assay			IC50=15.92 nM	SANGER
JAR	Growth Inhibition Assay			IC50=16.13 nM	SANGER
TGW	Growth Inhibition Assay			IC50=16.48 nM	SANGER
U-87-MG	Growth Inhibition Assay			IC50=16.76 nM	SANGER
NCI-H1436	Growth Inhibition Assay			IC50=17.01 nM	SANGER
GOTO	Growth Inhibition Assay			IC50=17.06 nM	SANGER
COLO-800	Growth Inhibition Assay			IC50=17.64 nM	SANGER
MFM-223	Growth Inhibition Assay			IC50=17.91 nM	SANGER
EW-18	Growth Inhibition Assay			IC50=17.96 nM	SANGER
NB14	Growth Inhibition Assay			IC50=17.98 nM	SANGER
EB2	Growth Inhibition Assay			IC50=18.08 nM	SANGER
EoL-1-	Growth Inhibition Assay			IC50=18.31 nM	SANGER
NCCIT	Growth Inhibition Assay			IC50=18.36 nM	SANGER
DG-75	Growth Inhibition Assay			IC50=18.61 nM	SANGER
HCC2218	Growth Inhibition Assay			IC50=19.5 nM	SANGER
TE-6	Growth Inhibition Assay			IC50=20.08 nM	SANGER
SF539	Growth Inhibition Assay			IC50=20.67 nM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=21.18 nM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=22.77 nM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=23.02 nM	SANGER
HCC2157	Growth Inhibition Assay			IC50=23.13 nM	SANGER
EW-12	Growth Inhibition Assay			IC50=23.17 nM	SANGER
SIMA	Growth Inhibition Assay			IC50=23.38 nM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=23.45 nM	SANGER
IM-9	Growth Inhibition Assay			IC50=23.54 nM	SANGER
EC-GI-10	Growth Inhibition Assay			IC50=24.23 nM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=24.54 nM	SANGER
LS-1034	Growth Inhibition Assay			IC50=25.75 nM	SANGER
REH	Growth Inhibition Assay			IC50=26.41 nM	SANGER
LU-165	Growth Inhibition Assay			IC50=26.72 nM	SANGER
NH-12	Growth Inhibition Assay			IC50=27.67 nM	SANGER
WSU-NHL	Growth Inhibition Assay			IC50=28.39 nM	SANGER
ECC4	Growth Inhibition Assay			IC50=28.79 nM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=29.69 nM	SANGER
EW-3	Growth Inhibition Assay			IC50=30.59 nM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=32.54 nM	SANGER
NCI-H719	Growth Inhibition Assay			IC50=34.31 nM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=35.04 nM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=35.17 nM	SANGER
ES3	Growth Inhibition Assay			IC50=35.19 nM	SANGER
UACC-812	Growth Inhibition Assay			IC50=35.44 nM	SANGER
C8166	Growth Inhibition Assay			IC50=35.7 nM	SANGER
MDA-MB-134-VI	Growth Inhibition Assay			IC50=35.87 nM	SANGER
D-283MED	Growth Inhibition Assay			IC50=37.79 nM	SANGER
SHP-77	Growth Inhibition Assay			IC50=38.03 nM	SANGER
NCI-H2227	Growth Inhibition Assay			IC50=40.49 nM	SANGER
SKM-1	Growth Inhibition Assay			IC50=42.63 nM	SANGER
L-428	Growth Inhibition Assay			IC50=43.86 nM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=45.89 nM	SANGER
NCI-H716	Growth Inhibition Assay			IC50=48.81 nM	SANGER
DMS-79	Growth Inhibition Assay			IC50=50.71 nM	SANGER
RS4-11	Growth Inhibition Assay			IC50=50.88 nM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=51.11 nM	SANGER
MC-CAR	Growth Inhibition Assay			IC50=51.52 nM	SANGER
TALL-1	Growth Inhibition Assay			IC50=53.91 nM	SANGER
NCI-N87	Growth Inhibition Assay			IC50=54.18 nM	SANGER
P30-OHK	Growth Inhibition Assay			IC50=54.61 nM	SANGER
LP-1	Growth Inhibition Assay			IC50=61.28 nM	SANGER
YT	Growth Inhibition Assay			IC50=61.8 nM	SANGER
MRK-nu-1	Growth Inhibition Assay			IC50=61.82 nM	SANGER
BT-474	Growth Inhibition Assay			IC50=65 nM	SANGER
NCI-H322M	Growth Inhibition Assay			IC50=66.11 nM	SANGER
NCI-H128	Growth Inhibition Assay			IC50=74.77 nM	SANGER
KMS-12-PE	Growth Inhibition Assay			IC50=76.24 nM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=76.74 nM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=77.66 nM	SANGER
EW-13	Growth Inhibition Assay			IC50=77.76 nM	SANGER
EW-11	Growth Inhibition Assay			IC50=78.52 nM	SANGER
SK-N-FI	Growth Inhibition Assay			IC50=80.2 nM	SANGER
CAL-148	Growth Inhibition Assay			IC50=81.84 nM	SANGER
RL	Growth Inhibition Assay			IC50=86.09 nM	SANGER
AM-38	Growth Inhibition Assay			IC50=88.08 nM	SANGER
RH-1	Growth Inhibition Assay			IC50=99.85 nM	SANGER
NCI-H1770	Growth Inhibition Assay			IC50=102.49 nM	SANGER
SIG-M5	Growth Inhibition Assay			IC50=105.06 nM	SANGER
GR-ST	Growth Inhibition Assay			IC50=113.34 nM	SANGER
ST486	Growth Inhibition Assay			IC50=114.06 nM	SANGER
NCI-H1650	Growth Inhibition Assay			IC50=115.29 nM	SANGER
MHH-CALL-2	Growth Inhibition Assay			IC50=115.7 nM	SANGER
BV-173	Growth Inhibition Assay			IC50=122.71 nM	SANGER
MC116	Growth Inhibition Assay			IC50=148.85 nM	SANGER
NCI-H524	Growth Inhibition Assay			IC50=159.1 nM	SANGER
SCLC-21H	Growth Inhibition Assay			IC50=159.41 nM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=169.21 nM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=185.37 nM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=196.52 nM	SANGER
KM-H2	Growth Inhibition Assay			IC50=197.05 nM	SANGER
NCI-H1395	Growth Inhibition Assay			IC50=210.13 nM	SANGER
NCI-H1155	Growth Inhibition Assay			IC50=230.32 nM	SANGER
COR-L279	Growth Inhibition Assay			IC50=252.17 nM	SANGER
NCI-H1299	Growth Inhibition Assay			IC50=261.71 nM	SANGER
EW-22	Growth Inhibition Assay			IC50=263.75 nM	SANGER
SK-MEL-2	Growth Inhibition Assay			IC50=281.9 nM	SANGER
KASUMI-1	Growth Inhibition Assay			IC50=283.05 nM	SANGER
NCI-H187	Growth Inhibition Assay			IC50=287.08 nM	SANGER
NCI-H2171	Growth Inhibition Assay			IC50=288.92 nM	SANGER
LNCaP-Clone-FGC	Growth Inhibition Assay			IC50=295.26 nM	SANGER
NCI-H1522	Growth Inhibition Assay			IC50=307.05 nM	SANGER
SCH	Growth Inhibition Assay			IC50=322.22 nM	SANGER
THP-1	Growth Inhibition Assay			IC50=322.6 nM	SANGER
SNU-C1	Growth Inhibition Assay			IC50=362.09 nM	SANGER
CA46	Growth Inhibition Assay			IC50=373.63 nM	SANGER
NCI-H1963	Growth Inhibition Assay			IC50=386.19 nM	SANGER
DEL	Growth Inhibition Assay			IC50=391.27 nM	SANGER
TUR	Growth Inhibition Assay			IC50=396.61 nM	SANGER
NCI-H226	Growth Inhibition Assay			IC50=403.23 nM	SANGER
COLO-668	Growth Inhibition Assay			IC50=403.57 nM	SANGER
CPC-N	Growth Inhibition Assay			IC50=403.77 nM	SANGER
NCI-H889	Growth Inhibition Assay			IC50=461.92 nM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=532.57 nM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=574.26 nM	SANGER
SCC-15	Growth Inhibition Assay			IC50=667.47 nM	SANGER
SUP-T1	Growth Inhibition Assay			IC50=686.04 nM	SANGER
DMS-153	Growth Inhibition Assay			IC50=746.83 nM	SANGER
MS-1	Growth Inhibition Assay			IC50=759.42 nM	SANGER
TC-YIK	Growth Inhibition Assay			IC50=781.01 nM	SANGER
RPMI-8866	Growth Inhibition Assay			IC50=1006.28 μM	SANGER
KY821	Growth Inhibition Assay			IC50=1036.04 μM	SANGER
P31-FUJ	Growth Inhibition Assay			IC50=1112.75 μM	SANGER
COLO-824	Growth Inhibition Assay			IC50=1261.78 μM	SANGER
U-698-M	Growth Inhibition Assay			IC50=2262.15 μM	SANGER
TE-441-T	Growth Inhibition Assay			IC50=2521.7 μM	SANGER
IMR-5	Growth Inhibition Assay			IC50=3409.62 μM	SANGER
NCI-H1838	Growth Inhibition Assay			IC50=4186.32 μM	SANGER
NCI-H2141	Growth Inhibition Assay			IC50=4.05 nM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=3.93 nM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=3.93 nM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=3.92 nM	SANGER
RL95-2	Growth Inhibition Assay			IC50=3.79 nM	SANGER
LC-1F	Growth Inhibition Assay			IC50=3.74 nM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=3.68 nM	SANGER
COLO-684	Growth Inhibition Assay			IC50=3.66 nM	SANGER
DJM-1	Growth Inhibition Assay			IC50=3.63 nM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=3.6 nM	SANGER
no-11	Growth Inhibition Assay			IC50=3.55 nM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=3.54 nM	SANGER
HCC1187	Growth Inhibition Assay			IC50=3.54 nM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=3.54 nM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=3.5 nM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=3.5 nM	SANGER
MEG-01	Growth Inhibition Assay			IC50=3.49 nM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=3.49 nM	SANGER
COR-L88	Growth Inhibition Assay			IC50=3.47 nM	SANGER
TE-15	Growth Inhibition Assay			IC50=3.43 nM	SANGER
DB	Growth Inhibition Assay			IC50=3.41 nM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=3.4 nM	SANGER
NEC8	Growth Inhibition Assay			IC50=3.35 nM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=3.26 nM	SANGER
CW-2	Growth Inhibition Assay			IC50=3.21 nM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=3.14 nM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=3.1 nM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=3.1 nM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=3.06 nM	SANGER
HT	Growth Inhibition Assay			IC50=3.02 nM	SANGER
SW954	Growth Inhibition Assay			IC50=2.9 nM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=2.89 nM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=2.89 nM	SANGER
ETK-1	Growth Inhibition Assay			IC50=2.84 nM	SANGER
CTV-1	Growth Inhibition Assay			IC50=2.8 nM	SANGER
EW-16	Growth Inhibition Assay			IC50=2.75 nM	SANGER
Mo-T	Growth Inhibition Assay			IC50=2.74 nM	SANGER
EB-3	Growth Inhibition Assay			IC50=2.66 nM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=2.57 nM	SANGER
KNS-81-FD	Growth Inhibition Assay			IC50=2.48 nM	SANGER
NB69	Growth Inhibition Assay			IC50=2.46 nM	SANGER
NCI-H64	Growth Inhibition Assay			IC50=2.44 nM	SANGER
KU812	Growth Inhibition Assay			IC50=2.42 nM	SANGER
NCI-H748	Growth Inhibition Assay			IC50=2.39 nM	SANGER
ARH-77	Growth Inhibition Assay			IC50=2.38 nM	SANGER
SCC-3	Growth Inhibition Assay			IC50=2.37 nM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=2.35 nM	SANGER
NB10	Growth Inhibition Assay			IC50=2.32 nM	SANGER
BC-1	Growth Inhibition Assay			IC50=2.31 nM	SANGER
NB5	Growth Inhibition Assay			IC50=2.27 nM	SANGER
KMOE-2	Growth Inhibition Assay			IC50=2.23 nM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=2.21 nM	SANGER
ES4	Growth Inhibition Assay			IC50=2.16 nM	SANGER
KGN	Growth Inhibition Assay			IC50=2.15 nM	SANGER
EKVX	Growth Inhibition Assay			IC50=2.14 nM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=2.13 nM	SANGER
KE-37	Growth Inhibition Assay			IC50=2.13 nM	SANGER
HH	Growth Inhibition Assay			IC50=2.13 nM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=2.12 nM	SANGER
BL-70	Growth Inhibition Assay			IC50=2.12 nM	SANGER
NOS-1	Growth Inhibition Assay			IC50=2.11 nM	SANGER
EW-24	Growth Inhibition Assay			IC50=2.08 nM	SANGER
LAN-6	Growth Inhibition Assay			IC50=2.05 nM	SANGER
NB17	Growth Inhibition Assay			IC50=2.04 nM	SANGER
LS-123	Growth Inhibition Assay			IC50=2.02 nM	SANGER
NB13	Growth Inhibition Assay			IC50=2 nM	SANGER
NKM-1	Growth Inhibition Assay			IC50=2 nM	SANGER
697	Growth Inhibition Assay			IC50=1.99 nM	SANGER
BE-13	Growth Inhibition Assay			IC50=1.93 nM	SANGER
MPP-89	Growth Inhibition Assay			IC50=1.89 nM	SANGER
Becker	Growth Inhibition Assay			IC50=1.83 nM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=1.82 nM	SANGER
GB-1	Growth Inhibition Assay			IC50=1.81 nM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=1.8 nM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=1.8 nM	SANGER
LC4-1	Growth Inhibition Assay			IC50=1.79 nM	SANGER
U-266	Growth Inhibition Assay			IC50=1.76 nM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=1.72 nM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=1.71 nM	SANGER
EHEB	Growth Inhibition Assay			IC50=1.67 nM	SANGER
GCIY	Growth Inhibition Assay			IC50=1.62 nM	SANGER
HEL	Growth Inhibition Assay			IC50=1.61 nM	SANGER
NB12	Growth Inhibition Assay			IC50=1.56 nM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=1.54 nM	SANGER
LS-411N	Growth Inhibition Assay			IC50=1.53 nM	SANGER
PF-382	Growth Inhibition Assay			IC50=1.47 nM	SANGER
CAS-1	Growth Inhibition Assay			IC50=1.37 nM	SANGER
L-540	Growth Inhibition Assay			IC50=1.37 nM	SANGER
ECC12	Growth Inhibition Assay			IC50=1.37 nM	SANGER
DU-4475	Growth Inhibition Assay			IC50=1.36 nM	SANGER
OPM-2	Growth Inhibition Assay			IC50=1.33 nM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=1.31 nM	SANGER
Calu-6	Growth Inhibition Assay			IC50=1.29 nM	SANGER
CMK	Growth Inhibition Assay			IC50=1.29 nM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=1.28 nM	SANGER
K5	Growth Inhibition Assay			IC50=1.28 nM	SANGER
KM12	Growth Inhibition Assay			IC50=1.27 nM	SANGER
SR	Growth Inhibition Assay			IC50=1.25 nM	SANGER
BL-41	Growth Inhibition Assay			IC50=1.25 nM	SANGER
Daudi	Growth Inhibition Assay			IC50=1.22 nM	SANGER
NCI-H1882	Growth Inhibition Assay			IC50=1.2 nM	SANGER
TE-8	Growth Inhibition Assay			IC50=1.19 nM	SANGER
HAL-01	Growth Inhibition Assay			IC50=1.18 nM	SANGER
EM-2	Growth Inhibition Assay			IC50=1.16 nM	SANGER
CCRF-CEM	Growth Inhibition Assay			IC50=1.13 nM	SANGER
D-392MG	Growth Inhibition Assay			IC50=1.1 nM	SANGER
MZ7-mel	Growth Inhibition Assay			IC50=1.09 nM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=1.09 nM	SANGER
SK-MM-2	Growth Inhibition Assay			IC50=1.09 nM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=1.08 nM	SANGER
RKO	Growth Inhibition Assay			IC50=1.06 nM	SANGER
TE-10	Growth Inhibition Assay			IC50=1.03 nM	SANGER
TE-1	Growth Inhibition Assay			IC50=1.03 nM	SANGER
PSN1	Growth Inhibition Assay			IC50=1.01 nM	SANGER
SW872	Growth Inhibition Assay			IC50=0.996 nM	SANGER
HC-1	Growth Inhibition Assay			IC50=0.975 nM	SANGER
KALS-1	Growth Inhibition Assay			IC50=0.925 nM	SANGER
SF268	Growth Inhibition Assay			IC50=0.923 nM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=0.917 nM	SANGER
RXF393	Growth Inhibition Assay			IC50=0.914 nM	SANGER
SNB75	Growth Inhibition Assay			IC50=0.912 nM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=0.895 nM	SANGER
TE-5	Growth Inhibition Assay			IC50=0.865 nM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=0.889 nM	SANGER
SK-LMS-1	Growth Inhibition Assay			IC50=0.854 nM	SANGER
SW684	Growth Inhibition Assay			IC50=0.821 nM	SANGER
ML-2	Growth Inhibition Assay			IC50=0.821 nM	SANGER
D-263MG	Growth Inhibition Assay			IC50=0.807 nM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=0.804 nM	SANGER
GI-1	Growth Inhibition Assay			IC50=0.764 nM	SANGER
ES7	Growth Inhibition Assay			IC50=0.766 nM	SANGER
LS-513	Growth Inhibition Assay			IC50=0.739 nM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=0.722 nM	SANGER
UACC-257	Growth Inhibition Assay			IC50=0.71 nM	SANGER
LB373-MEL-D	Growth Inhibition Assay			IC50=0.7 nM	SANGER
SF126	Growth Inhibition Assay			IC50=0.701 nM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=0.693 nM	SANGER
TK10	Growth Inhibition Assay			IC50=0.679 nM	SANGER
D-336MG	Growth Inhibition Assay			IC50=0.657 nM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=0.652 nM	SANGER
HOP-62	Growth Inhibition Assay			IC50=0.647 nM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=0.641 nM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=0.634 nM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=0.623 nM	SANGER
HT-144	Growth Inhibition Assay			IC50=0.576 nM	SANGER
COLO-829	Growth Inhibition Assay			IC50=0.614 nM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=0.539 nM	SANGER
CESS	Growth Inhibition Assay			IC50=0.538 nM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=0.533 nM	SANGER
DSH1	Growth Inhibition Assay			IC50=0.48 nM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=0.474 nM	SANGER
CP66-MEL	Growth Inhibition Assay			IC50=0.473 nM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=0.447 nM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=0.443 nM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=0.44 nM	SANGER
HCE-T	Growth Inhibition Assay			IC50=0.439 nM	SANGER
ES1	Growth Inhibition Assay			IC50=0.43 nM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=0.425 nM	SANGER
ACN	Growth Inhibition Assay			IC50=0.417 nM	SANGER
D-247MG	Growth Inhibition Assay			IC50=0.413 nM	SANGER
HCC2998	Growth Inhibition Assay			IC50=0.412 nM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=0.407 nM	SANGER
ES8	Growth Inhibition Assay			IC50=0.4 nM	SANGER
A388	Growth Inhibition Assay			IC50=0.356 nM	SANGER
KS-1	Growth Inhibition Assay			IC50=0.34 nM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.335 nM	SANGER
ONS-76	Growth Inhibition Assay			IC50=0.33 nM	SANGER
D-542MG	Growth Inhibition Assay			IC50=0.329 nM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=0.304 nM	SANGER
LOUCY	Growth Inhibition Assay			IC50=0.293 nM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=0.289 nM	SANGER
LXF-289	Growth Inhibition Assay			IC50=0.269 nM	SANGER
KNS-42	Growth Inhibition Assay			IC50=0.258 nM	SANGER
8-MG-BA	Growth Inhibition Assay			IC50=0.25 nM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=0.243 nM	SANGER
A101D	Growth Inhibition Assay			IC50=0.225 nM	SANGER
MMAC-SF	Growth Inhibition Assay			IC50=0.216 nM	SANGER
no-10	Growth Inhibition Assay			IC50=0.21 nM	SANGER
A253	Growth Inhibition Assay			IC50=0.208 nM	SANGER
TE-9	Growth Inhibition Assay			IC50=0.182 nM	SANGER
SH-4	Growth Inhibition Assay			IC50=0.173 nM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=0.163 nM	SANGER
ES6	Growth Inhibition Assay			IC50=0.0021 nM	SANGER
Molt4	Function assay			EC50 = 0.021 μM	18247547
Molt4	Function assay			EC50 = 0.021 μM	22503349
RPMI8226	Growth inhibition assay			GI50 = 0.00023 μM	24946214
CCRF-CEM	Growth inhibition assay			GI50 = 0.00035 μM	24946214
MDA-MB-435	Growth inhibition assay			GI50 = 0.00044 μM	24946214
MALME-3M	Growth inhibition assay			GI50 = 0.00045 μM	24946214
NCI-H226	Growth inhibition assay			GI50 = 0.00046 μM	24946214
SK-MEL-28	Growth inhibition assay			GI50 = 0.00046 μM	24946214
A498	Growth inhibition assay			GI50 = 0.00048 μM	24946214
MOLT4	Growth inhibition assay			GI50 = 0.00051 μM	24946214
OVCAR3	Growth inhibition assay			GI50 = 0.00054 μM	24946214
SW620	Growth inhibition assay			GI50 = 0.00055 μM	24946214
MCF7	Growth inhibition assay			GI50 = 0.00055 μM	24946214
BT549	Growth inhibition assay			GI50 = 0.00055 μM	24946214
UACC257	Growth inhibition assay			GI50 = 0.00059 μM	24946214
SF539	Growth inhibition assay			GI50 = 0.00059 μM	24946214
HCC2998	Growth inhibition assay			GI50 = 0.0006 μM	24946214
HCT116	Growth inhibition assay			GI50 = 0.0006 μM	24946214
T47D	Growth inhibition assay			GI50 = 0.0006 μM	24946214
CAKI-1	Growth inhibition assay			GI50 = 0.00066 μM	24946214
SK-MEL-5	Growth inhibition assay			GI50 = 0.00068 μM	24946214
RXF393	Growth inhibition assay			GI50 = 0.00071 μM	24946214
LOXIMVI	Growth inhibition assay			GI50 = 0.00078 μM	24946214
ACHN	Growth inhibition assay			GI50 = 0.00079 μM	24946214
SR	Growth inhibition assay			GI50 = 0.00085 μM	24946214
UACC62	Growth inhibition assay			GI50 = 0.00091 μM	24946214
M14	Growth inhibition assay			GI50 = 0.00093 μM	24946214
HT-29	Growth inhibition assay			GI50 = 0.00095 μM	24946214
HOP92	Growth inhibition assay			GI50 = 0.001 μM	24946214
NCI-H23	Growth inhibition assay			GI50 = 0.001 μM	24946214
TK10	Growth inhibition assay			GI50 = 0.001 μM	24946214
Hs 578T	Growth inhibition assay			GI50 = 0.00102 μM	24946214
UO31	Growth inhibition assay			GI50 = 0.00105 μM	24946214
SK-MEL-2	Growth inhibition assay			GI50 = 0.00107 μM	24946214
SN12C	Growth inhibition assay			GI50 = 0.0011 μM	24946214
K562	Growth inhibition assay			GI50 = 0.00117 μM	24946214
SF268	Growth inhibition assay			GI50 = 0.00117 μM	24946214
COLO205	Growth inhibition assay			GI50 = 0.00123 μM	24946214
MDA-MB-231	Growth inhibition assay			GI50 = 0.00126 μM	24946214
NCI-H522	Growth inhibition assay			GI50 = 0.00144 μM	24946214
786-0	Growth inhibition assay			GI50 = 0.00144 μM	24946214
MDA-MB-468	Growth inhibition assay			GI50 = 0.00148 μM	24946214
HCT15	Growth inhibition assay			GI50 = 0.00151 μM	24946214
U251	Growth inhibition assay			GI50 = 0.00155 μM	24946214
OVCAR5	Growth inhibition assay			GI50 = 0.00155 μM	24946214
KM12	Growth inhibition assay			GI50 = 0.0017 μM	24946214
SF295	Growth inhibition assay			GI50 = 0.0017 μM	24946214
DU145	Growth inhibition assay			GI50 = 0.0017 μM	24946214
HL-60(TB)	Growth inhibition assay			GI50 = 0.0019 μM	24946214
OVCAR4	Growth inhibition assay			GI50 = 0.00195 μM	24946214
SNB19	Growth inhibition assay			GI50 = 0.00204 μM	24946214
SNB75	Growth inhibition assay			GI50 = 0.00204 μM	24946214
IGROV1	Growth inhibition assay			GI50 = 0.00224 μM	24946214
OVCAR8	Growth inhibition assay			GI50 = 0.00263 μM	24946214
PC3	Growth inhibition assay			GI50 = 0.00263 μM	24946214
EKVX	Growth inhibition assay			GI50 = 0.00302 μM	24946214
A549/ATCC	Growth inhibition assay			GI50 = 0.00309 μM	24946214
HOP62	Growth inhibition assay			GI50 = 0.00447 μM	24946214
NCI-H460	Growth inhibition assay			GI50 = 0.00447 μM	24946214
NCI-ADR-RES	Growth inhibition assay			GI50 = 0.0123 μM	24946214
SKOV3	Growth inhibition assay			GI50 = 0.0138 μM	24946214
NCI-H322M	Growth inhibition assay			GI50 = 0.0178 μM	24946214
A2780	Cytotoxicity assay			IC50 = 0.0017 μM	18247547
RPMI8226	Cytotoxicity assay			IC50 = 0.0088 μM	20727746
HCT116	Function assay			Inhibition of proteasome in human HCT116 cells assessed as accumulation of p53 by Western blotting analysis	23547757
HCT116	Apoptosis assay			Induction of apoptosis in human HCT116 cells assessed as induction of PARP cleavage by Western blotting analysis	23547757
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
fibroblast	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
fibroblast	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
HepG2	Cell viability assay			HepG2 cells viability qHTS for Zika virus inhibitors	33229545
点击查看更多细胞系数据

生物活性

产品描述

靶点

NF-κB ^[6]	20S proteasome ^[1] (Cell-free assay)
	0.6 nM(Ki)

体外研究(In Vitro)
体外研究活性	Bortezomib，一种硼酸二肽，是一种26S蛋白酶体的高选择性可逆抑制剂，其作用于错误折叠蛋白的降解，并且对细胞周期的调控是必要的。暴露于Bortezomib能够稳定p21，p27，和p53，以及促凋亡Bid和Bax蛋白，微囊蛋白-1，和抑制剂κB-α，这防止了核因子κB诱导的细胞存活途径的激活。Bortezomib也会促进促凋亡c-Jun-NH2末端激酶，以及内质网应激反应的激活。这些细胞蛋白水平的改变导致对增殖，迁移的抑制，和癌细胞凋亡的促进。^[2] Bortezomib能够渗透到细胞，并抑制蛋白酶体介导的细胞内长寿蛋白水解，抑制50%蛋白质水解的浓度为∼0.1 μM。Bortezomib对衍生自美国国家癌症研究所(NCI)多重人类肿瘤的一组60个癌细胞系的IC50值为7 nM。PC-3细胞用Bortezomib (100 nM)处理8小时导致细胞积聚在G2-M期，相应的G1期细胞数量减少。Bortezomib在24和48小时杀死PC-3细胞，IC50分别为100和20 nM。Bortezomib治疗16-24小时后诱导细胞核缩合。Bortezomib在低至100 nM浓度下以时间依赖的方式导致PARP裂解，在处理24小时后产生效果。^[1]
激酶实验	动力学法
激酶实验	在典型的动力学试验中，2.00 mL试验缓冲液(20 mM HEPES，0.5 mM EDTA，0.035% SDS，pH 7.8) 和 Suc-Leu-Leu-Val-Tyr-AMC溶于DMSO，加入3 mL荧光比色皿中，并将比色皿放置于荧光分光光度计的夹套细胞皿座。反应温度通过循环水浴维持在37℃。反应溶液达到热平衡后(5 分钟)，1 μL−10 μL储存酶溶液加入培养皿。伴随AMC 从多肽AMC底物裂解的反应进程通过440 nm (λex= 380 nm)下荧光发射的增加监测。
细胞实验	细胞系	人多发性骨髓瘤细胞系U266
	浓度	~10 μM
	孵育时间	2天
	方法	通过测定细胞吸收 MTT染料的情况而测定 Bortezomib对 MM和 BMSC 生长的抑制情况。每孔使用10 μL 5 mg/mL MTT对培养48小时的细胞进行脉冲处理，至少处理4小时，随后加入100 μL 含0.04 N HCl的异丙醇。使用分光光度计在 570 nm处测定吸光值。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	phospho-PERK / ATF-4 GRP-78 / GADD-34 pro-caspase-12 / pro-caspase-3 pro-caspase-9 p-IκBα / IκBα COX-2 / cIAP2		15509775
	Immunofluorescence	Vimentin Ubiquitin		19010849
	Growth inhibition assay	Cell viability		20571067
	ELISA	IL-8		24085292

体内研究(In Vivo)
体内研究活性	Bortezomib单一用药的抗癌作用已在多发性骨髓瘤的异种移植模型，成人白血病，肺癌，乳腺癌，前列腺癌，胰腺癌，头颈癌，和结肠癌，以及在黑色素瘤中得到证实。^[2]在Lewis肺癌模型中，口服bortezomib (1.0 mg/ kg，每天)，服用18天引起肿瘤生长延迟，并减少转移数量。Bortezomib单一用药，高达5 mg/kg剂量时显著降低乳腺癌细胞的存活率。在前列腺癌小鼠异种移植模型中，Bortezomib (1.0 mg/kg，每周一次)用药4周减少60%肿瘤生长。1.0 mg/kg Bortezomib给药4周导致胰腺癌小鼠异种移植物生长减少72%或84%，并导致肿瘤细胞凋亡增加。1.0 mg/kg Bortezomib显著抑制人浆细胞瘤异种移植物生长，增加肿瘤细胞凋亡和总存活率，并减少肿瘤血管生成。^[3]
动物实验	Animal Models	人浆细胞瘤异种移植物RPMI 8226
	Dosages	1mg/kg
	Administration	i.v.，一周两次，使用4周，然后一周一次

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05599880	Recruiting	Relapsed/Refractory Immune Thrombocytopenia	Seoul National University Hospital	July 7 2023	Phase 2
NCT05781425	Recruiting	Chemotherapy-induced Peripheral Neuropathy	Odense University Hospital\|Aarhus University Hospital\|Sygehus Lillebaelt\|University of Southern Denmark	May 12 2023	--
NCT05383547	Unknown status	Bortezomib\|Glomerulonephritis\|MN\|MPGN\|FSGS\|IgA Nephropathy	Ruijin Hospital	August 2 2022	Not Applicable
NCT04915248	Recruiting	Plasmablastic Lymphoma	Fondazione Italiana Linfomi - ETS\|Janssen-Cilag S.p.A.	July 11 2022	Phase 2
NCT04656951	Recruiting	Multiple Myeloma	University of Cologne\|Janssen-Cilag G.m.b.H	June 1 2021	Phase 2

参考文献
[1] Adams J, et al. Cancer Res, 1999, 59(11), 2615-2622. [2] Boccadoro M, et al. Cancer Cell Int, 2005, 5(1):18. [3] LeBlanc R, et al. Cancer Res, 2002, 62(17), 4996-5000 [4] Stein RL, et al. Biochemistry. 1996, 35(13), 3899-3908. [5] Hideshima T, et al. Cancer Res, 2001, 61(7), 3071-3076. [6] Mohammad A Shahshahan, et al. Am J Cancer Res . 2011;1(7):913-24. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	384.24	分子式	C₁₉H₂₅BN₄O₄
CAS号	179324-69-7	SDF	Download Bortezomib SDF
Smiles	B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
储存条件(自收到货起)	3年 -20°C(避光) 粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年 -20°C(避光) 粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 77 mg/mL ( (200.39 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 77 mg/mL ( (200.39 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL ( (197.79 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	2.000mg/ml (5.21mM)	以 1 mL 工作液为例，取 50 μL 40 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀使其澄清；向上述体系中加入50 μL Tween-80，混合均匀使其澄清；然后继续加入 500 μLddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (13.01mM)	以 1 mL 工作液为例，取 50 μL 100 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀使其澄清；向上述体系中加入50 μL Tween-80，混合均匀使其澄清；然后继续加入 500 μLddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
On your website, it is mentioned that Bortezomib should be prepared at a concentration of 5 mg/ml in 2% DMSO/30% PEG300/ddH2O for in vivo use. But on the product sheet we received with the compound, it is mentioned: 5mg/ml in 0.5% methylcellulose, 0.2% tween 80. So which is the correct preparation buffer?

回答：
S1013 Bortezomib in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml is a clear solution, and it in 0.5% methylcellulose+0.2% Tween 80 is a suspension. Please choose the suitable vehicle according to your administration route. When you prepare the clear solution, please dissolve Bortezomib in DMSO first, make sure it dissolves well, warm it up to 45 degree and/or sonicate if necessary, then add PEG, mix well, and finally add water.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Bortezomib

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常见问题及建议解决方法