Palbociclib Isethionate

别名: PD0332991 Isethionate

Palbociclib Isethionate是一种高度选择性的CDK4/6抑制剂,无细胞试验中IC50为11 nM/16 nM,对CDK1/2/5,EGFR,FGFR,PDGFR, InsR等没有抑制活性。Phase 3。

Palbociclib Isethionate Chemical Structure

Palbociclib Isethionate Chemical Structure

CAS: 827022-33-3

规格 价格 库存 购买数量
10mg RMB 1217.51 现货
25mg RMB 2189.47 现货
50mg RMB 3026.06 现货
200mg RMB 4316.13 现货
1g RMB 7944.3 现货
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400-668-6834

info@selleck.cn

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客户使用Selleck的Palbociclib Isethionate发表文献277

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批次: 纯度: 99.99%
99.99

Palbociclib Isethionate相关产品

相关信号通路图

CDK抑制剂选择性比较

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
U-CH6 Growth Inhibition Assay 0-1 μM 72 h IC50=90 nM 26183925
U-CH3 Growth Inhibition Assay 0-1 μM 72 h IC50=52 nM 26183925
U-CH2 Growth Inhibition Assay 0-1 μM 72 h IC50=50.2 nM 26183925
IMR-32 Fuction Assay 0-1 μM 24 h reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner 26225123
NGP Fuction Assay 0-1 μM 24 h reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner 26225123
SH-EP Growth Inhibition Assay 1 μM 24 h induces G1 arrest 26225123
NGP Growth Inhibition Assay 1 μM 24 h induces G1 arrest 26225123
SH-SY5Y Growth Inhibition Assay 1 μM 24 h induces G1 arrest 26225123
IMR-32 Growth Inhibition Assay 1 μM 24 h induces G1 arrest 26225123
H596 Growth Inhibition Assay 0-100 μM 72 h IC50=12 μM 26390342
H520 Growth Inhibition Assay 0-100 μM 72 h IC50=0.73 μM 26390342
H2170 Growth Inhibition Assay 0-100 μM 72 h IC50=5 μM 26390342
H157 Growth Inhibition Assay 0-100 μM 72 h IC50=9 μM 26390342
U-CH7 Growth Inhibition Assay 0-1 μM 72 h IC50=98 nM 26183925
U-CH11 Growth Inhibition Assay 0-1 μM 72 h IC50=340 nM 26183925
MCF7 Fuction Assay 2.5-250 nM 24 h reduces Rb phosphorylation 25991817
MV4-11 Apoptosis Assay 0.5 μM 24 h enhances apoptosis induced by sorafenib and AC220 25487917
MOLM13 Apoptosis Assay 0.5 μM 24 h enhances apoptosis induced by sorafenib and AC220 25487917
MCF7 Antitumor assay 100 mg/kg/day 14 days Antitumor activity against human estrogen-independent human MCF7 cells xenografted in RNU rat assessed as tumor growth inhibition at 100 mg/kg/day, ig administered for 14 days measured on day 15 27448913
MDA-MB-231 Cell cycle arrest assay 0.5 to 1 uM 24 hrs Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis 24417566
MCF7 Cell cycle arrest assay 0.5 to 1 uM 24 hrs Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis 24417566
MDA-MB-231 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MDA-MB-231 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MCF7 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
MCF7 Function assay 0.5 to 5 uM 24 hrs Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis 24417566
SH-EP Growth Inhibition Assay 48 h IC50=2.211 μM 26225123
NGP Growth Inhibition Assay 48 h IC50=2.077 μM 26225123
SH-SY5Y Growth Inhibition Assay 48 h IC50=676 nM 26225123
IMR-32 Growth Inhibition Assay 48 h IC50=261 nM 26225123
MOLM13 Function assay 24 hrs Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs, IC50 = 0.011 μM. 24641103
COLO205 Antiproliferative assay 72 hrs Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.036 μM. 24641103
MOLM13 Antiproliferative assay 72 hrs Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. 24641103
MOLM13 Antiproliferative assay 72 hrs Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. 24641103
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.14 μM. 24641103
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. 26115571
MDA-MB-435 Antiproliferative assay 24 hrs Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis, IC50 = 0.16 μM. 26115571
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. 27171036
insect cell Function assay 2 mins Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. 27171036
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. 27171036
insect cell Function assay 2 mins Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. 27171036
MDA-MB-453 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.137 μM. 27448913
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.24 μM. 27448913
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.58 μM. 27448913
A2780 Growth inhibition assay 72 hrs Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.032 μM. 28156111
MV4-11 Growth inhibition assay 72 hrs Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50 = 0.05 μM. 28156111
MOLM13 Growth inhibition assay 72 hrs Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.062 μM. 28156111
NB4 Growth inhibition assay 72 hrs Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.066 μM. 28156111
PC3 Growth inhibition assay 72 hrs Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.071 μM. 28156111
MDA-MB-453 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay, GI50 = 0.326 μM. 28156111
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.557 μM. 28156111
M229 Growth inhibition assay 72 hrs Growth inhibition of human M229 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.22 μM. 28156111
M238 Growth inhibition assay 72 hrs Growth inhibition of human M238 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.97 μM. 28156111
M249 Growth inhibition assay 72 hrs Growth inhibition of human M249 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.99 μM. 28156111
M249R Growth inhibition assay 72 hrs Growth inhibition of human M249R cells after 72 hrs by resazurin or MTT assay, GI50 = 2.96 μM. 28156111
C4-2B Growth inhibition assay 72 hrs Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay, GI50 = 4.15 μM. 28156111
DU145 Growth inhibition assay 72 hrs Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.792 μM. 28156111
MDA-MB-468 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.96 μM. 28156111
BPH1 Growth inhibition assay 72 hrs Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay, GI50 = 7.442 μM. 28156111
K562 Cytotoxicity assay 96 hrs Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 2 μM. 24417566
DU145 Cytotoxicity assay 96 hrs Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 7.5 μM. 24417566
MV4-11 Function assay 12 to 24 hrs Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis 28156111
MV4-11 Function assay 12 to 24 hrs Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis 28156111
MOLM13-ITD alone Growth Inhibition Assay IC50=0.089 ± 0.009 μM 25487917
MV4-11-ITD alone Growth Inhibition Assay IC50=0.092 ± 0.008 μM 25487917
MOLM13-ITD/D835Y Growth Inhibition Assay IC50=0.114 ± 0.011 μM 25487917
MV4-11-ITD/D835V Growth Inhibition Assay IC50=0.116 ± 0.011 μM 25487917
MV4-11-ITD/D835V Growth Inhibition Assay IC50=0.102 ± 0.006 μM 25487917
MV4-11-ITD/F691L Growth Inhibition Assay IC50=0.112 ± 0.015 μM 25487917
MV4-11-ITD/N841K Growth Inhibition Assay IC50=0.113 ± 0.002 μM 25487917
U937-FLT3 WT Growth Inhibition Assay IC50=0.102 ± 0.013 μM 25487917
P12-ICHIKAWA Growth Inhibition assay IC50 = 0.09604 μM SANGER
697 Growth Inhibition assay IC50 = 0.14838 μM SANGER
NB69 Growth Inhibition assay IC50 = 0.1618 μM SANGER
EoL-1-cell Growth Inhibition assay IC50 = 0.18726 μM SANGER
BHT-101 Growth Inhibition assay IC50 = 0.19825 μM SANGER
SK-NEP-1 Growth Inhibition assay IC50 = 0.22002 μM SANGER
MHH-NB-11 Growth Inhibition assay IC50 = 0.22019 μM SANGER
AsPC-1 Growth Inhibition assay IC50 = 0.25253 μM SANGER
ES1 Growth Inhibition assay IC50 = 0.25625 μM SANGER
LAMA-84 Growth Inhibition assay IC50 = 0.25819 μM SANGER
MOLT-16 Growth Inhibition assay IC50 = 0.25849 μM SANGER
ES7 Growth Inhibition assay IC50 = 0.27309 μM SANGER
KY821 Growth Inhibition assay IC50 = 0.3141 μM SANGER
RT-112 Growth Inhibition assay IC50 = 0.32105 μM SANGER
HL-60 Growth Inhibition assay IC50 = 0.34066 μM SANGER
MOLT-4 Growth Inhibition assay IC50 = 0.34513 μM SANGER
KARPAS-45 Growth Inhibition assay IC50 = 0.37616 μM SANGER
SK-N-AS Growth Inhibition assay IC50 = 0.38783 μM SANGER
CTB-1 Growth Inhibition assay IC50 = 0.40502 μM SANGER
NKM-1 Growth Inhibition assay IC50 = 0.41189 μM SANGER
HTC-C3 Growth Inhibition assay IC50 = 0.43295 μM SANGER
BE-13 Growth Inhibition assay IC50 = 0.44427 μM SANGER
KOSC-2 Growth Inhibition assay IC50 = 0.4669 μM SANGER
NB14 Growth Inhibition assay IC50 = 0.48358 μM SANGER
CAL-27 Growth Inhibition assay IC50 = 0.49459 μM SANGER
H9 Growth Inhibition assay IC50 = 0.49543 μM SANGER
RS4-11 Growth Inhibition assay IC50 = 0.50473 μM SANGER
PA-1 Growth Inhibition assay IC50 = 0.50986 μM SANGER
MV-4-11 Growth Inhibition assay IC50 = 0.51385 μM SANGER
OS-RC-2 Growth Inhibition assay IC50 = 0.52162 μM SANGER
RPMI-8226 Growth Inhibition assay IC50 = 0.52686 μM SANGER
HGC-27 Growth Inhibition assay IC50 = 0.56499 μM SANGER
CHP-212 Growth Inhibition assay IC50 = 0.59359 μM SANGER
NB10 Growth Inhibition assay IC50 = 0.59918 μM SANGER
HH Growth Inhibition assay IC50 = 0.59943 μM SANGER
EW-16 Growth Inhibition assay IC50 = 0.60352 μM SANGER
ES8 Growth Inhibition assay IC50 = 0.60521 μM SANGER
HAL-01 Growth Inhibition assay IC50 = 0.60567 μM SANGER
A204 Growth Inhibition assay IC50 = 0.63391 μM SANGER
MHH-PREB-1 Growth Inhibition assay IC50 = 0.63699 μM SANGER
EM-2 Growth Inhibition assay IC50 = 0.65064 μM SANGER
BV-173 Growth Inhibition assay IC50 = 0.65248 μM SANGER
ONS-76 Growth Inhibition assay IC50 = 0.67782 μM SANGER
KM-H2 Growth Inhibition assay IC50 = 0.69554 μM SANGER
D-263MG Growth Inhibition assay IC50 = 0.71712 μM SANGER
ES3 Growth Inhibition assay IC50 = 0.72893 μM SANGER
VA-ES-BJ Growth Inhibition assay IC50 = 0.73227 μM SANGER
NBsusSR Growth Inhibition assay IC50 = 0.74299 μM SANGER
NCI-H520 Growth Inhibition assay IC50 = 0.74652 μM SANGER
ES5 Growth Inhibition assay IC50 = 0.7528 μM SANGER
T-24 Growth Inhibition assay IC50 = 0.77871 μM SANGER
SW962 Growth Inhibition assay IC50 = 0.80863 μM SANGER
EW-3 Growth Inhibition assay IC50 = 0.80876 μM SANGER
RXF393 Growth Inhibition assay IC50 = 0.81279 μM SANGER
U251 Growth Inhibition assay IC50 = 0.81388 μM SANGER
CAMA-1 Growth Inhibition assay IC50 = 0.83394 μM SANGER
JVM-3 Growth Inhibition assay IC50 = 0.85178 μM SANGER
COLO-800 Growth Inhibition assay IC50 = 0.89778 μM SANGER
OVCAR-5 Growth Inhibition assay IC50 = 0.9001 μM SANGER
LB1047-RCC Growth Inhibition assay IC50 = 0.92756 μM SANGER
SW954 Growth Inhibition assay IC50 = 0.92941 μM SANGER
J-RT3-T3-5 Growth Inhibition assay IC50 = 0.93606 μM SANGER
Mewo Growth Inhibition assay IC50 = 0.9366 μM SANGER
NCI-H1770 Growth Inhibition assay IC50 = 0.94055 μM SANGER
HO-1-N-1 Growth Inhibition assay IC50 = 0.96281 μM SANGER
HSC-3 Growth Inhibition assay IC50 = 0.96648 μM SANGER
TYK-nu Growth Inhibition assay IC50 = 0.99825 μM SANGER
KYSE-150 Growth Inhibition assay IC50 = 1.00076 μM SANGER
SN12C Growth Inhibition assay IC50 = 1.00875 μM SANGER
MOLT-13 Growth Inhibition assay IC50 = 1.01421 μM SANGER
TE-11 Growth Inhibition assay IC50 = 1.04812 μM SANGER
DB Growth Inhibition assay IC50 = 1.07273 μM SANGER
CAL-39 Growth Inhibition assay IC50 = 1.07522 μM SANGER
A3-KAW Growth Inhibition assay IC50 = 1.08408 μM SANGER
CHP-134 Growth Inhibition assay IC50 = 1.11807 μM SANGER
TGW Growth Inhibition assay IC50 = 1.12395 μM SANGER
QIMR-WIL Growth Inhibition assay IC50 = 1.13134 μM SANGER
NCI-SNU-1 Growth Inhibition assay IC50 = 1.16354 μM SANGER
CGTH-W-1 Growth Inhibition assay IC50 = 1.17186 μM SANGER
MHH-ES-1 Growth Inhibition assay IC50 = 1.17986 μM SANGER
LB2241-RCC Growth Inhibition assay IC50 = 1.1862 μM SANGER
ML-2 Growth Inhibition assay IC50 = 1.20734 μM SANGER
COR-L23 Growth Inhibition assay IC50 = 1.22933 μM SANGER
BFTC-905 Growth Inhibition assay IC50 = 1.24267 μM SANGER
Hs-578-T Growth Inhibition assay IC50 = 1.25817 μM SANGER
KG-1 Growth Inhibition assay IC50 = 1.26686 μM SANGER
HEL Growth Inhibition assay IC50 = 1.29338 μM SANGER
A549 Growth Inhibition assay IC50 = 1.29399 μM SANGER
COLO-741 Growth Inhibition assay IC50 = 1.32089 μM SANGER
PC-3 Growth Inhibition assay IC50 = 1.35221 μM SANGER
HOS Growth Inhibition assay IC50 = 1.35296 μM SANGER
HT-1080 Growth Inhibition assay IC50 = 1.37519 μM SANGER
TE-8 Growth Inhibition assay IC50 = 1.41774 μM SANGER
BHY Growth Inhibition assay IC50 = 1.46923 μM SANGER
BB65-RCC Growth Inhibition assay IC50 = 1.50528 μM SANGER
HN Growth Inhibition assay IC50 = 1.54071 μM SANGER
NCI-H441 Growth Inhibition assay IC50 = 1.54907 μM SANGER
RPMI-8866 Growth Inhibition assay IC50 = 1.58507 μM SANGER
CAL-62 Growth Inhibition assay IC50 = 1.60862 μM SANGER
MG-63 Growth Inhibition assay IC50 = 1.61813 μM SANGER
SK-LU-1 Growth Inhibition assay IC50 = 1.62152 μM SANGER
BCPAP Growth Inhibition assay IC50 = 1.66457 μM SANGER
22RV1 Growth Inhibition assay IC50 = 1.67843 μM SANGER
T47D Growth Inhibition assay IC50 = 1.68061 μM SANGER
MSTO-211H Growth Inhibition assay IC50 = 1.69603 μM SANGER
DEL Growth Inhibition assay IC50 = 1.70273 μM SANGER
H4 Growth Inhibition assay IC50 = 1.73212 μM SANGER
CAL-51 Growth Inhibition assay IC50 = 1.74855 μM SANGER
ABC-1 Growth Inhibition assay IC50 = 1.78582 μM SANGER
MZ2-MEL Growth Inhibition assay IC50 = 1.79542 μM SANGER
YKG-1 Growth Inhibition assay IC50 = 1.81061 μM SANGER
KM12 Growth Inhibition assay IC50 = 1.81602 μM SANGER
L-363 Growth Inhibition assay IC50 = 1.87412 μM SANGER
KU812 Growth Inhibition assay IC50 = 1.89282 μM SANGER
LOXIMVI Growth Inhibition assay IC50 = 1.91228 μM SANGER
G-401 Growth Inhibition assay IC50 = 1.92428 μM SANGER
SW780 Growth Inhibition assay IC50 = 1.96246 μM SANGER
SW872 Growth Inhibition assay IC50 = 1.9833 μM SANGER
NB7 Growth Inhibition assay IC50 = 1.99323 μM SANGER
T98G Growth Inhibition assay IC50 = 2.00666 μM SANGER
SW1710 Growth Inhibition assay IC50 = 2.06945 μM SANGER
NCI-H1573 Growth Inhibition assay IC50 = 2.07298 μM SANGER
KE-37 Growth Inhibition assay IC50 = 2.08951 μM SANGER
786-0 Growth Inhibition assay IC50 = 2.15439 μM SANGER
SAS Growth Inhibition assay IC50 = 2.20374 μM SANGER
CAL-54 Growth Inhibition assay IC50 = 2.20413 μM SANGER
SF268 Growth Inhibition assay IC50 = 2.23122 μM SANGER
SW620 Growth Inhibition assay IC50 = 2.26169 μM SANGER
MN-60 Growth Inhibition assay IC50 = 2.3106 μM SANGER
EFO-27 Growth Inhibition assay IC50 = 2.32058 μM SANGER
NCI-H747 Growth Inhibition assay IC50 = 2.32199 μM SANGER
HCC2218 Growth Inhibition assay IC50 = 2.35374 μM SANGER
MIA-PaCa-2 Growth Inhibition assay IC50 = 2.36437 μM SANGER
SJSA-1 Growth Inhibition assay IC50 = 2.37796 μM SANGER
RKO Growth Inhibition assay IC50 = 2.38496 μM SANGER
NB6 Growth Inhibition assay IC50 = 2.40374 μM SANGER
ES4 Growth Inhibition assay IC50 = 2.45422 μM SANGER
EGI-1 Growth Inhibition assay IC50 = 2.46883 μM SANGER
CTV-1 Growth Inhibition assay IC50 = 2.52773 μM SANGER
NCI-H1355 Growth Inhibition assay IC50 = 2.55951 μM SANGER
GT3TKB Growth Inhibition assay IC50 = 2.59199 μM SANGER
SK-HEP-1 Growth Inhibition assay IC50 = 2.59266 μM SANGER
GAMG Growth Inhibition assay IC50 = 2.59394 μM SANGER
SK-MES-1 Growth Inhibition assay IC50 = 2.61803 μM SANGER
RO82-W-1 Growth Inhibition assay IC50 = 2.62057 μM SANGER
ECC10 Growth Inhibition assay IC50 = 2.70206 μM SANGER
MCF7 Growth Inhibition assay IC50 = 2.71464 μM SANGER
D-283MED Growth Inhibition assay IC50 = 2.7243 μM SANGER
RPMI-7951 Growth Inhibition assay IC50 = 2.75694 μM SANGER
Ramos-2G6-4C10 Growth Inhibition assay IC50 = 2.77099 μM SANGER
KGN Growth Inhibition assay IC50 = 2.81884 μM SANGER
NUGC-3 Growth Inhibition assay IC50 = 2.82505 μM SANGER
NCI-H292 Growth Inhibition assay IC50 = 2.85053 μM SANGER
Becker Growth Inhibition assay IC50 = 2.95832 μM SANGER
NCI-H1299 Growth Inhibition assay IC50 = 3.05263 μM SANGER
ETK-1 Growth Inhibition assay IC50 = 3.0543 μM SANGER
TK10 Growth Inhibition assay IC50 = 3.20165 μM SANGER
VMRC-RCZ Growth Inhibition assay IC50 = 3.36488 μM SANGER
YH-13 Growth Inhibition assay IC50 = 3.44079 μM SANGER
DU-145 Growth Inhibition assay IC50 = 3.46269 μM SANGER
SW1088 Growth Inhibition assay IC50 = 3.4747 μM SANGER
HOP-92 Growth Inhibition assay IC50 = 3.50342 μM SANGER
KP-N-YS Growth Inhibition assay IC50 = 3.62139 μM SANGER
NCI-H460 Growth Inhibition assay IC50 = 3.6673 μM SANGER
U-2-OS Growth Inhibition assay IC50 = 3.72535 μM SANGER
A101D Growth Inhibition assay IC50 = 3.76936 μM SANGER
MDA-MB-231 Growth Inhibition assay IC50 = 3.81951 μM SANGER
IST-MES1 Growth Inhibition assay IC50 = 3.832 μM SANGER
COR-L105 Growth Inhibition assay IC50 = 4.018 μM SANGER
NCI-H1437 Growth Inhibition assay IC50 = 4.02302 μM SANGER
CAL-85-1 Growth Inhibition assay IC50 = 4.02461 μM SANGER
MZ1-PC Growth Inhibition assay IC50 = 4.18556 μM SANGER
VM-CUB-1 Growth Inhibition assay IC50 = 4.31284 μM SANGER
CHL-1 Growth Inhibition assay IC50 = 4.32169 μM SANGER
MDA-MB-361 Growth Inhibition assay IC50 = 4.33153 μM SANGER
NCI-H661 Growth Inhibition assay IC50 = 4.50092 μM SANGER
EW-11 Growth Inhibition assay IC50 = 4.52231 μM SANGER
BEN Growth Inhibition assay IC50 = 4.52815 μM SANGER
BFTC-909 Growth Inhibition assay IC50 = 4.56275 μM SANGER
NCI-H2087 Growth Inhibition assay IC50 = 4.58164 μM SANGER
RVH-421 Growth Inhibition assay IC50 = 4.6669 μM SANGER
P30-OHK Growth Inhibition assay IC50 = 4.68008 μM SANGER
NCI-H28 Growth Inhibition assay IC50 = 4.81661 μM SANGER
ES6 Growth Inhibition assay IC50 = 4.83016 μM SANGER
769-P Growth Inhibition assay IC50 = 4.85926 μM SANGER
OE33 Growth Inhibition assay IC50 = 4.88161 μM SANGER
SW982 Growth Inhibition assay IC50 = 4.95061 μM SANGER
A388 Growth Inhibition assay IC50 = 5.02983 μM SANGER
TI-73 Growth Inhibition assay IC50 = 5.06194 μM SANGER
HCT-116 Growth Inhibition assay IC50 = 5.09889 μM SANGER
HuP-T3 Growth Inhibition assay IC50 = 5.18709 μM SANGER
G-402 Growth Inhibition assay IC50 = 5.19416 μM SANGER
NCI-H1792 Growth Inhibition assay IC50 = 5.24622 μM SANGER
NCI-H209 Growth Inhibition assay IC50 = 5.25942 μM SANGER
NCI-H1650 Growth Inhibition assay IC50 = 5.30634 μM SANGER
LCLC-97TM1 Growth Inhibition assay IC50 = 5.31808 μM SANGER
S-117 Growth Inhibition assay IC50 = 5.36976 μM SANGER
GI-ME-N Growth Inhibition assay IC50 = 5.39681 μM SANGER
NCI-H2122 Growth Inhibition assay IC50 = 5.49397 μM SANGER
NCI-H1793 Growth Inhibition assay IC50 = 5.67593 μM SANGER
C2BBe1 Growth Inhibition assay IC50 = 5.70088 μM SANGER
TE-12 Growth Inhibition assay IC50 = 5.80556 μM SANGER
LCLC-103H Growth Inhibition assay IC50 = 5.917 μM SANGER
A673 Growth Inhibition assay IC50 = 5.91932 μM SANGER
BB30-HNC Growth Inhibition assay IC50 = 5.9836 μM SANGER
SF295 Growth Inhibition assay IC50 = 6.00422 μM SANGER
KU-19-19 Growth Inhibition assay IC50 = 6.01731 μM SANGER
CFPAC-1 Growth Inhibition assay IC50 = 6.04443 μM SANGER
LoVo Growth Inhibition assay IC50 = 6.05063 μM SANGER
8505C Growth Inhibition assay IC50 = 6.07573 μM SANGER
GMS-10 Growth Inhibition assay IC50 = 6.15002 μM SANGER
Ca9-22 Growth Inhibition assay IC50 = 6.1671 μM SANGER
DOK Growth Inhibition assay IC50 = 6.22072 μM SANGER
FADU Growth Inhibition assay IC50 = 6.26039 μM SANGER
BxPC-3 Growth Inhibition assay IC50 = 6.2732 μM SANGER
CAL-33 Growth Inhibition assay IC50 = 6.29201 μM SANGER
SHP-77 Growth Inhibition assay IC50 = 6.31512 μM SANGER
LXF-289 Growth Inhibition assay IC50 = 6.33455 μM SANGER
GB-1 Growth Inhibition assay IC50 = 6.382 μM SANGER
KS-1 Growth Inhibition assay IC50 = 6.38447 μM SANGER
D-502MG Growth Inhibition assay IC50 = 6.42376 μM SANGER
LAN-6 Growth Inhibition assay IC50 = 6.51023 μM SANGER
H-EMC-SS Growth Inhibition assay IC50 = 6.56147 μM SANGER
LC-2-ad Growth Inhibition assay IC50 = 6.60076 μM SANGER
NCI-H1693 Growth Inhibition assay IC50 = 6.62215 μM SANGER
SK-N-FI Growth Inhibition assay IC50 = 6.75044 μM SANGER
D-423MG Growth Inhibition assay IC50 = 6.76117 μM SANGER
KNS-42 Growth Inhibition assay IC50 = 6.78197 μM SANGER
GCT Growth Inhibition assay IC50 = 6.938 μM SANGER
DSH1 Growth Inhibition assay IC50 = 7.0633 μM SANGER
D-247MG Growth Inhibition assay IC50 = 7.07881 μM SANGER
NCI-SNU-5 Growth Inhibition assay IC50 = 7.18371 μM SANGER
TE-6 Growth Inhibition assay IC50 = 7.20601 μM SANGER
NOMO-1 Growth Inhibition assay IC50 = 7.22127 μM SANGER
NB17 Growth Inhibition assay IC50 = 7.30309 μM SANGER
EW-22 Growth Inhibition assay IC50 = 7.34348 μM SANGER
EW-13 Growth Inhibition assay IC50 = 7.35162 μM SANGER
DOHH-2 Growth Inhibition assay IC50 = 7.4402 μM SANGER
TGBC1TKB Growth Inhibition assay IC50 = 7.49899 μM SANGER
GR-ST Growth Inhibition assay IC50 = 7.52594 μM SANGER
KYSE-520 Growth Inhibition assay IC50 = 7.55515 μM SANGER
CAPAN-1 Growth Inhibition assay IC50 = 7.5951 μM SANGER
HCE-4 Growth Inhibition assay IC50 = 7.62279 μM SANGER
MLMA Growth Inhibition assay IC50 = 7.62957 μM SANGER
HT-144 Growth Inhibition assay IC50 = 7.65368 μM SANGER
KYSE-180 Growth Inhibition assay IC50 = 7.71169 μM SANGER
TE-5 Growth Inhibition assay IC50 = 7.95971 μM SANGER
IGROV-1 Growth Inhibition assay IC50 = 7.98551 μM SANGER
NCI-H1581 Growth Inhibition assay IC50 = 8.012 μM SANGER
SW1990 Growth Inhibition assay IC50 = 8.04659 μM SANGER
EFM-19 Growth Inhibition assay IC50 = 8.08545 μM SANGER
IGR-1 Growth Inhibition assay IC50 = 8.43023 μM SANGER
U-118-MG Growth Inhibition assay IC50 = 8.43463 μM SANGER
SK-OV-3 Growth Inhibition assay IC50 = 8.46765 μM SANGER
KNS-62 Growth Inhibition assay IC50 = 8.51761 μM SANGER
GOTO Growth Inhibition assay IC50 = 8.57635 μM SANGER
8305C Growth Inhibition assay IC50 = 8.70484 μM SANGER
RPMI-2650 Growth Inhibition assay IC50 = 8.71955 μM SANGER
NEC8 Growth Inhibition assay IC50 = 8.74307 μM SANGER
KYSE-450 Growth Inhibition assay IC50 = 8.86548 μM SANGER
RMG-I Growth Inhibition assay IC50 = 9.14058 μM SANGER
CAKI-1 Growth Inhibition assay IC50 = 9.31979 μM SANGER
KYSE-510 Growth Inhibition assay IC50 = 9.35778 μM SANGER
A4-Fuk Growth Inhibition assay IC50 = 9.36701 μM SANGER
AN3-CA Growth Inhibition assay IC50 = 9.45444 μM SANGER
SK-N-DZ Growth Inhibition assay IC50 = 9.72849 μM SANGER
HSC-2 Growth Inhibition assay IC50 = 9.76629 μM SANGER
EW-1 Growth Inhibition assay IC50 = 9.79369 μM SANGER
D-566MG Growth Inhibition assay IC50 = 9.83664 μM SANGER
COLO-792 Growth Inhibition assay IC50 = 9.98746 μM SANGER
TE-10 Growth Inhibition assay IC50 = 10.0396 μM SANGER
NCI-H650 Growth Inhibition assay IC50 = 10.4286 μM SANGER
U-266 Growth Inhibition assay IC50 = 10.455 μM SANGER
Detroit562 Growth Inhibition assay IC50 = 11.0515 μM SANGER
NH-12 Growth Inhibition assay IC50 = 11.1446 μM SANGER
OC-314 Growth Inhibition assay IC50 = 11.2842 μM SANGER
IST-MEL1 Growth Inhibition assay IC50 = 11.5323 μM SANGER
KNS-81-FD Growth Inhibition assay IC50 = 11.5527 μM SANGER
SW1463 Growth Inhibition assay IC50 = 11.5989 μM SANGER
NCI-H23 Growth Inhibition assay IC50 = 11.6553 μM SANGER
SK-MEL-2 Growth Inhibition assay IC50 = 11.7197 μM SANGER
NB13 Growth Inhibition assay IC50 = 12.1495 μM SANGER
Daoy Growth Inhibition assay IC50 = 12.2855 μM SANGER
NCI-H1623 Growth Inhibition assay IC50 = 12.3801 μM SANGER
NMC-G1 Growth Inhibition assay IC50 = 12.717 μM SANGER
DK-MG Growth Inhibition assay IC50 = 12.9482 μM SANGER
TCCSUP Growth Inhibition assay IC50 = 13.1284 μM SANGER
SCC-15 Growth Inhibition assay IC50 = 13.2651 μM SANGER
NOS-1 Growth Inhibition assay IC50 = 13.2893 μM SANGER
RH-1 Growth Inhibition assay IC50 = 13.3037 μM SANGER
SK-MEL-3 Growth Inhibition assay IC50 = 13.3728 μM SANGER
NB5 Growth Inhibition assay IC50 = 13.4067 μM SANGER
SNU-387 Growth Inhibition assay IC50 = 13.5072 μM SANGER
CAL-120 Growth Inhibition assay IC50 = 13.6718 μM SANGER
LNCaP-Clone-FGC Growth Inhibition assay IC50 = 13.7991 μM SANGER
ACN Growth Inhibition assay IC50 = 14.0288 μM SANGER
SK-MEL-30 Growth Inhibition assay IC50 = 14.063 μM SANGER
COLO-678 Growth Inhibition assay IC50 = 14.0822 μM SANGER
SCC-9 Growth Inhibition assay IC50 = 14.1021 μM SANGER
KINGS-1 Growth Inhibition assay IC50 = 14.1402 μM SANGER
LS-513 Growth Inhibition assay IC50 = 14.187 μM SANGER
HLE Growth Inhibition assay IC50 = 14.3852 μM SANGER
SW1573 Growth Inhibition assay IC50 = 14.4435 μM SANGER
KYSE-140 Growth Inhibition assay IC50 = 14.6327 μM SANGER
SK-PN-DW Growth Inhibition assay IC50 = 14.8001 μM SANGER
A253 Growth Inhibition assay IC50 = 15.0625 μM SANGER
CAL-12T Growth Inhibition assay IC50 = 15.4662 μM SANGER
COLO-679 Growth Inhibition assay IC50 = 15.7683 μM SANGER
UACC-257 Growth Inhibition assay IC50 = 16.1201 μM SANGER
U-87-MG Growth Inhibition assay IC50 = 16.3523 μM SANGER
HCC1806 Growth Inhibition assay IC50 = 16.7071 μM SANGER
NCI-H2170 Growth Inhibition assay IC50 = 17.2448 μM SANGER
AGS Growth Inhibition assay IC50 = 17.3808 μM SANGER
MEL-HO Growth Inhibition assay IC50 = 17.7503 μM SANGER
SW48 Growth Inhibition assay IC50 = 17.7716 μM SANGER
HuP-T4 Growth Inhibition assay IC50 = 18.0206 μM SANGER
NCI-H720 Growth Inhibition assay IC50 = 18.1402 μM SANGER
RCC10RGB Growth Inhibition assay IC50 = 18.1697 μM SANGER
HD-MY-Z Growth Inhibition assay IC50 = 18.2254 μM SANGER
A427 Growth Inhibition assay IC50 = 18.5094 μM SANGER
HCC2998 Growth Inhibition assay IC50 = 18.6051 μM SANGER
EPLC-272H Growth Inhibition assay IC50 = 19.0434 μM SANGER
C32 Growth Inhibition assay IC50 = 19.045 μM SANGER
UMC-11 Growth Inhibition assay IC50 = 19.2123 μM SANGER
CaR-1 Growth Inhibition assay IC50 = 19.6804 μM SANGER
KYSE-410 Growth Inhibition assay IC50 = 19.9139 μM SANGER
HuCCT1 Growth Inhibition assay IC50 = 20.6293 μM SANGER
LB996-RCC Growth Inhibition assay IC50 = 20.7168 μM SANGER
KYSE-70 Growth Inhibition assay IC50 = 20.8059 μM SANGER
CAL-72 Growth Inhibition assay IC50 = 20.915 μM SANGER
Capan-2 Growth Inhibition assay IC50 = 21.0413 μM SANGER
PANC-08-13 Growth Inhibition assay IC50 = 21.2515 μM SANGER
SBC-1 Growth Inhibition assay IC50 = 21.3081 μM SANGER
MFM-223 Growth Inhibition assay IC50 = 21.3342 μM SANGER
BB49-HNC Growth Inhibition assay IC50 = 21.5716 μM SANGER
SH-4 Growth Inhibition assay IC50 = 21.6618 μM SANGER
HuO9 Growth Inhibition assay IC50 = 21.9825 μM SANGER
AM-38 Growth Inhibition assay IC50 = 22.0485 μM SANGER
A431 Growth Inhibition assay IC50 = 23.2119 μM SANGER
YAPC Growth Inhibition assay IC50 = 23.2651 μM SANGER
LU-139 Growth Inhibition assay IC50 = 23.4809 μM SANGER
HEC-1 Growth Inhibition assay IC50 = 23.4937 μM SANGER
SCC-25 Growth Inhibition assay IC50 = 24.3006 μM SANGER
HT-29 Growth Inhibition assay IC50 = 24.3823 μM SANGER
PC-14 Growth Inhibition assay IC50 = 24.6571 μM SANGER
Calu-6 Growth Inhibition assay IC50 = 25.5071 μM SANGER
SJRH30 Growth Inhibition assay IC50 = 25.6496 μM SANGER
ChaGo-K-1 Growth Inhibition assay IC50 = 26.1629 μM SANGER
IA-LM Growth Inhibition assay IC50 = 26.3645 μM SANGER
GP5d Growth Inhibition assay IC50 = 26.4491 μM SANGER
NCI-H2291 Growth Inhibition assay IC50 = 26.6541 μM SANGER
BALL-1 Growth Inhibition assay IC50 = 26.9397 μM SANGER
HCC1954 Growth Inhibition assay IC50 = 26.9808 μM SANGER
NCI-H2452 Growth Inhibition assay IC50 = 27.4163 μM SANGER
LU-99A Growth Inhibition assay IC50 = 27.5582 μM SANGER
NTERA-S-cl-D1 Growth Inhibition assay IC50 = 27.7299 μM SANGER
PANC-10-05 Growth Inhibition assay IC50 = 27.7775 μM SANGER
NCI-H2405 Growth Inhibition assay IC50 = 27.9387 μM SANGER
MDA-MB-415 Growth Inhibition assay IC50 = 28.4137 μM SANGER
NCI-H2342 Growth Inhibition assay IC50 = 28.5281 μM SANGER
TGBC24TKB Growth Inhibition assay IC50 = 28.7117 μM SANGER
LU-134-A Growth Inhibition assay IC50 = 28.9261 μM SANGER
SCC-4 Growth Inhibition assay IC50 = 31.0495 μM SANGER
Saos-2 Growth Inhibition assay IC50 = 31.9306 μM SANGER
RERF-LC-MS Growth Inhibition assay IC50 = 32.8231 μM SANGER
M14 Growth Inhibition assay IC50 = 32.9764 μM SANGER
HPAF-II Growth Inhibition assay IC50 = 33.5011 μM SANGER
NCI-H1755 Growth Inhibition assay IC50 = 34.3305 μM SANGER
D-392MG Growth Inhibition assay IC50 = 35.8674 μM SANGER
A704 Growth Inhibition assay IC50 = 36.0427 μM SANGER
CP50-MEL-B Growth Inhibition assay IC50 = 36.1911 μM SANGER
EW-18 Growth Inhibition assay IC50 = 36.452 μM SANGER
WM-115 Growth Inhibition assay IC50 = 36.8099 μM SANGER
LU-65 Growth Inhibition assay IC50 = 37.1417 μM SANGER
NCI-H1563 Growth Inhibition assay IC50 = 37.2484 μM SANGER
DBTRG-05MG Growth Inhibition assay IC50 = 38.0691 μM SANGER
NCI-H630 Growth Inhibition assay IC50 = 38.4714 μM SANGER
NCI-H1155 Growth Inhibition assay IC50 = 39.242 μM SANGER
OVCAR-3 Growth Inhibition assay IC50 = 39.9195 μM SANGER
OAW-42 Growth Inhibition assay IC50 = 40.4258 μM SANGER
JVM-2 Growth Inhibition assay IC50 = 41.2415 μM SANGER
C3A Growth Inhibition assay IC50 = 41.3447 μM SANGER
HT55 Growth Inhibition assay IC50 = 42.2841 μM SANGER
OVCAR-4 Growth Inhibition assay IC50 = 42.2974 μM SANGER
MEG-01 Growth Inhibition assay IC50 = 42.4616 μM SANGER
NCI-H82 Growth Inhibition assay IC50 = 43.9892 μM SANGER
JEG-3 Growth Inhibition assay IC50 = 44.947 μM SANGER
BPH-1 Growth Inhibition assay IC50 = 46.3998 μM SANGER
MPP-89 Growth Inhibition assay IC50 = 47.2898 μM SANGER
ALL-PO Growth Inhibition assay IC50 = 47.4188 μM SANGER
HT Growth Inhibition assay IC50 = 47.492 μM SANGER
NCI-H2347 Growth Inhibition assay IC50 = 48.0715 μM SANGER
A2780 Growth Inhibition assay IC50 = 49.4228 μM SANGER
KARPAS-299 Growth Inhibition assay IC50 = 49.5119 μM SANGER
NCI-H1651 Growth Inhibition assay IC50 = 49.8821 μM SANGER
OCI-AML2 Growth Inhibition assay IC50 = 50.2084 μM SANGER
OCUB-M Growth Inhibition assay IC50 = 50.3047 μM SANGER
HuH-7 Growth Inhibition assay IC50 = 50.5943 μM SANGER
RCM-1 Growth Inhibition assay IC50 = 50.9133 μM SANGER
FTC-133 Growth Inhibition assay IC50 = 51.322 μM SANGER
PSN1 Growth Inhibition assay IC50 = 51.4335 μM SANGER
A498 Growth Inhibition assay IC50 = 52.0995 μM SANGER
SF126 Growth Inhibition assay IC50 = 52.6568 μM SANGER
UACC-62 Growth Inhibition assay IC50 = 55.2224 μM SANGER
PANC-03-27 Growth Inhibition assay IC50 = 56.6788 μM SANGER
NCI-H727 Growth Inhibition assay IC50 = 56.8127 μM SANGER
SNU-423 Growth Inhibition assay IC50 = 57.2859 μM SANGER
LB771-HNC Growth Inhibition assay IC50 = 57.8405 μM SANGER
HCC1395 Growth Inhibition assay IC50 = 58.0464 μM SANGER
OAW-28 Growth Inhibition assay IC50 = 58.2785 μM SANGER
NB12 Growth Inhibition assay IC50 = 60.6696 μM SANGER
DJM-1 Growth Inhibition assay IC50 = 60.7331 μM SANGER
MDA-MB-157 Growth Inhibition assay IC50 = 61.1649 μM SANGER
DU-4475 Growth Inhibition assay IC50 = 62.5495 μM SANGER
RD Growth Inhibition assay IC50 = 62.7387 μM SANGER
LS-123 Growth Inhibition assay IC50 = 63.2618 μM SANGER
NCI-H226 Growth Inhibition assay IC50 = 64.22 μM SANGER
MS-1 Growth Inhibition assay IC50 = 64.8358 μM SANGER
no-10 Growth Inhibition assay IC50 = 65.7473 μM SANGER
SW626 Growth Inhibition assay IC50 = 65.7579 μM SANGER
DMS-273 Growth Inhibition assay IC50 = 66.2296 μM SANGER
ESS-1 Growth Inhibition assay IC50 = 66.5096 μM SANGER
TE-9 Growth Inhibition assay IC50 = 66.6316 μM SANGER
CAS-1 Growth Inhibition assay IC50 = 67.7954 μM SANGER
639-V Growth Inhibition assay IC50 = 69.4198 μM SANGER
GAK Growth Inhibition assay IC50 = 70.2031 μM SANGER
NCI-H526 Growth Inhibition assay IC50 = 71.0913 μM SANGER
DoTc2-4510 Growth Inhibition assay IC50 = 71.443 μM SANGER
647-V Growth Inhibition assay IC50 = 73.2118 μM SANGER
OVCAR-8 Growth Inhibition assay IC50 = 73.2367 μM SANGER
COLO-680N Growth Inhibition assay IC50 = 75.2497 μM SANGER
HDLM-2 Growth Inhibition assay IC50 = 75.7806 μM SANGER
TGBC11TKB Growth Inhibition assay IC50 = 79.0192 μM SANGER
DMS-114 Growth Inhibition assay IC50 = 81.9577 μM SANGER
CW-2 Growth Inhibition assay IC50 = 82.6818 μM SANGER
MDA-MB-175-VII Growth Inhibition assay IC50 = 85.3135 μM SANGER
HT-1376 Growth Inhibition assay IC50 = 85.846 μM SANGER
SW1417 Growth Inhibition assay IC50 = 88.2906 μM SANGER
HCE-T Growth Inhibition assay IC50 = 91.7205 μM SANGER
OE19 Growth Inhibition assay IC50 = 92.7944 μM SANGER
NCI-N87 Growth Inhibition assay IC50 = 92.8881 μM SANGER
SNU-449 Growth Inhibition assay IC50 = 93.584 μM SANGER
NCI-H1092 Growth Inhibition assay IC50 = 96.5851 μM SANGER
COLO-684 Growth Inhibition assay IC50 = 99.0686 μM SANGER
HCC1937 Growth Inhibition assay IC50 = 99.9315 μM SANGER
EFO-21 Growth Inhibition assay IC50 = 110.988 μM SANGER
ZR-75-30 Growth Inhibition assay IC50 = 114.117 μM SANGER
HCC1187 Growth Inhibition assay IC50 = 114.179 μM SANGER
SW684 Growth Inhibition assay IC50 = 114.655 μM SANGER
AU565 Growth Inhibition assay IC50 = 115.892 μM SANGER
HCC38 Growth Inhibition assay IC50 = 116.559 μM SANGER
LK-2 Growth Inhibition assay IC50 = 119.652 μM SANGER
LB2518-MEL Growth Inhibition assay IC50 = 122.428 μM SANGER
COLO-320-HSR Growth Inhibition assay IC50 = 126.212 μM SANGER
HCC1419 Growth Inhibition assay IC50 = 129.227 μM SANGER
NCI-H2228 Growth Inhibition assay IC50 = 129.321 μM SANGER
NCI-H2052 Growth Inhibition assay IC50 = 130.358 μM SANGER
HCC2157 Growth Inhibition assay IC50 = 133.973 μM SANGER
HCC1569 Growth Inhibition assay IC50 = 135.05 μM SANGER
HuO-3N1 Growth Inhibition assay IC50 = 135.366 μM SANGER
MZ7-mel Growth Inhibition assay IC50 = 145.604 μM SANGER
SW756 Growth Inhibition assay IC50 = 147.143 μM SANGER
NCI-H1304 Growth Inhibition assay IC50 = 149.222 μM SANGER
LN-405 Growth Inhibition assay IC50 = 149.732 μM SANGER
BT-474 Growth Inhibition assay IC50 = 150.969 μM SANGER
LS-411N Growth Inhibition assay IC50 = 152.319 μM SANGER
ATN-1 Growth Inhibition assay IC50 = 152.458 μM SANGER
SNU-C2B Growth Inhibition assay IC50 = 153.444 μM SANGER
KYSE-270 Growth Inhibition assay IC50 = 155.75 μM SANGER
NCI-H1395 Growth Inhibition assay IC50 = 156.493 μM SANGER
EKVX Growth Inhibition assay IC50 = 156.981 μM SANGER
HCC70 Growth Inhibition assay IC50 = 157.989 μM SANGER
NCI-H522 Growth Inhibition assay IC50 = 161.368 μM SANGER
Ca-Ski Growth Inhibition assay IC50 = 161.86 μM SANGER
SW1116 Growth Inhibition assay IC50 = 163.382 μM SANGER
8-MG-BA Growth Inhibition assay IC50 = 165.797 μM SANGER
NCI-H1048 Growth Inhibition assay IC50 = 172.374 μM SANGER
RH-18 Growth Inhibition assay IC50 = 172.601 μM SANGER
LU-135 Growth Inhibition assay IC50 = 173.259 μM SANGER
SW948 Growth Inhibition assay IC50 = 174.6 μM SANGER
LS-1034 Growth Inhibition assay IC50 = 183.742 μM SANGER
SCH Growth Inhibition assay IC50 = 187.022 μM SANGER
KP-N-YN Growth Inhibition assay IC50 = 192.971 μM SANGER
NCI-H69 Growth Inhibition assay IC50 = 210.925 μM SANGER
SBC-5 Growth Inhibition assay IC50 = 211.162 μM SANGER
MFE-280 Growth Inhibition assay IC50 = 212.067 μM SANGER
MC116 Growth Inhibition assay IC50 = 212.736 μM SANGER
BT-20 Growth Inhibition assay IC50 = 216.38 μM SANGER
NCI-H1993 Growth Inhibition assay IC50 = 217.295 μM SANGER
Calu-3 Growth Inhibition assay IC50 = 217.37 μM SANGER
GCIY Growth Inhibition assay IC50 = 221.332 μM SANGER
HT-3 Growth Inhibition assay IC50 = 222.173 μM SANGER
MC-IXC Growth Inhibition assay IC50 = 227.215 μM SANGER
COR-L88 Growth Inhibition assay IC50 = 234.259 μM SANGER
SK-MEL-1 Growth Inhibition assay IC50 = 235.59 μM SANGER
MDA-MB-453 Growth Inhibition assay IC50 = 236.33 μM SANGER
SiHa Growth Inhibition assay IC50 = 247.22 μM SANGER
C8166 Growth Inhibition assay IC50 = 251.341 μM SANGER
SKG-IIIa Growth Inhibition assay IC50 = 251.504 μM SANGER
HT-1197 Growth Inhibition assay IC50 = 268.492 μM SANGER
no-11 Growth Inhibition assay IC50 = 291.357 μM SANGER
ME-180 Growth Inhibition assay IC50 = 296.912 μM SANGER
NY Growth Inhibition assay IC50 = 320.632 μM SANGER
C-33-A Growth Inhibition assay IC50 = 325.06 μM SANGER
NCI-H2029 Growth Inhibition assay IC50 = 338.305 μM SANGER
IST-SL1 Growth Inhibition assay IC50 = 342.105 μM SANGER
KLE Growth Inhibition assay IC50 = 347.29 μM SANGER
SF539 Growth Inhibition assay IC50 = 348.01 μM SANGER
5637 Growth Inhibition assay IC50 = 360.37 μM SANGER
COLO-824 Growth Inhibition assay IC50 = 363.58 μM SANGER
NCI-H810 Growth Inhibition assay IC50 = 363.938 μM SANGER
JAR Growth Inhibition assay IC50 = 365.01 μM SANGER
L-428 Growth Inhibition assay IC50 = 369.277 μM SANGER
COLO-668 Growth Inhibition assay IC50 = 387.033 μM SANGER
GI-1 Growth Inhibition assay IC50 = 398.59 μM SANGER
NCI-H446 Growth Inhibition assay IC50 = 399.497 μM SANGER
CCRF-CEM Growth Inhibition assay IC50 = 403.587 μM SANGER
T84 Growth Inhibition assay IC50 = 403.686 μM SANGER
K-562 Growth Inhibition assay IC50 = 432.947 μM SANGER
OMC-1 Growth Inhibition assay IC50 = 433.814 μM SANGER
LB831-BLC Growth Inhibition assay IC50 = 434.556 μM SANGER
BT-549 Growth Inhibition assay IC50 = 435.102 μM SANGER
MKN7 Growth Inhibition assay IC50 = 439.822 μM SANGER
SW1783 Growth Inhibition assay IC50 = 449.251 μM SANGER
SNB75 Growth Inhibition assay IC50 = 486.478 μM SANGER
M059J Growth Inhibition assay IC50 = 492.923 μM SANGER
KURAMOCHI Growth Inhibition assay IC50 = 498.612 μM SANGER
TE-1 Growth Inhibition assay IC50 = 502.729 μM SANGER
NCI-H596 Growth Inhibition assay IC50 = 530.805 μM SANGER
PFSK-1 Growth Inhibition assay IC50 = 532.941 μM SANGER
sf9 Function assay Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. 26851505
sf9 Function assay Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. 26851505
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
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
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
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生物活性

产品描述 Palbociclib Isethionate是一种高度选择性的CDK4/6抑制剂,无细胞试验中IC50为11 nM/16 nM,对CDK1/2/5,EGFR,FGFR,PDGFR, InsR等没有抑制活性。Phase 3。
特性 PD 0332991治疗多种癌症,特异性抑制CDK4/6,是第一种有前途的抑制剂。
靶点
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
体外研究(In Vitro)
体外研究活性 PD 0332991对CDK4/6具有绝对选择性,对其他CDKs几乎没有抑制活性。PD 0332991作用于MDA-MB-435乳腺癌细胞,有效降低Rb在Ser780 和 Ser795位点磷酸化,IC50分别为66 nM和63 nM。PD 0332991通过抑制细胞进入S期,有效抑制细胞生长,抑制 DNA复制。PD 0332991抑制胸苷渗透进Rb阳性人类乳腺癌(如MDA-MB-435, MCF-7), 结肠癌 (H1299), 和肺癌(Colo-205) 及白血病(CRRF-CEM和K562)的DNA中,IC50值为0.04-0.17 μM。PD 0332991显著增强MDA-MB-453在G1期的百分比。[1]PD 0332991作用于CD138+原发性骨髓瘤细胞,初级非转化的B细胞,MM1.S和CAG HMCLs细胞系,抑制Rb磷酸化,IC50分别为 <0.1 μM, 0.05 μM, 和 60-70 nM。PD 0332991作用于CD138+原发性骨髓瘤细胞和初级非转化的B细胞,诱导细胞停滞在G1期。PD 0332991诱导MM1.S细胞停滞在G1期,IC50为~0.05 μM。[2]PD 0332991优先抑制Luminal雌激素受体阳性(包括HER2阳性)人类乳腺癌细胞系。PD 0332991作用于大部分敏感的细胞系,促进pRb和cyclin D1基因表达,且降低CDKN2A(p16)基因表达。PD 0332991作用于条件性抗ER抑制的细胞系,增强对Tamoxifen的敏感性。[3]
激酶实验 CDK活性实验
在96孔过滤板中进行动力学测评,测定CDK实验的IC50值。所有的CDK-cyclin激酶复合物在昆虫细胞中通过杆状病毒感染而表达,并进行纯化。实验底物是与GST(GST•RB-Cterm)融合的pRb组分(792–928位氨基酸)。总反应体积为0.1 mL,包含终浓度20 mM Tris-HCl,pH 7.4, 50 mM NaCl,1 mM 二硫苏糖醇,10 mM MgCl2,含0.25 μCi[γ-32P]ATP的25 μM ATP(作用于 CDK4-cyclin D1, CDK6-cyclin D2, 和 CDK6-cyclin D3), 20 ng 酶, 1 μg GST•RB-Cterm, 及适度稀释的抑制剂。每孔加入全部组分,除了[γ-32P]ATP,置于混合器中2分钟。加入[γ-32P]ATP开始反应,在25°C下温育15分钟。加入0.1 mL 20% 三氯乙酸终止反应, 实验板置于4°C至少1小时,使底物沉淀。每孔使用 0.2 mL 10%三氯乙酸洗涤 五次,使用β计数器测定渗透的放射性。
细胞实验 细胞系 人类乳腺癌细胞MDA-MB-435
浓度 2 μM
孵育时间 6 天
方法 细胞按一式两份每孔5,000 到10,000个细胞接种在24孔板中,接种后,加入不同浓度的PD 0332991。对照组不加入药物。温育末期,细胞胰蛋白酶化,并置于等渗溶液中,并立即使用Coulter Z2粒子计数器计数。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot RB1 (pT821) / RB1 (pS780) pAMPKα(T172) / AMPKα pULK1(S317) / ULK1 c-Jun / p-c-Jun / NFκB(p50) p38 / p-P38 / JNK / p-JNK 30300583
Growth inhibition assay Cell viability IC50 28453226
Immunofluorescence γH2AX(Ser139) LC3B 29669860
ELISA PGE2 26540629
体内研究(In Vivo)
体内研究活性 PD 0332991(150 mg/kg)作用于Colo-205结肠癌移植瘤,诱导肿瘤快速衰退,肿瘤生长相应延迟。PD 0332991(150 mg/kg)作用于MDA-MB-435乳腺癌,诱导全部肿瘤停滞和杀死细胞。PD 0332991(150 mg/kg)处理携带SF-295胶质母细胞瘤,和ZR-75-1乳腺癌和PC-3前列腺肿瘤模型(完全抑制肿瘤生长)的小鼠,显著诱导肿瘤衰退。PD 0332991 (150 mg/kg)处理 MDA-MB-435乳腺癌超过24小时,抑制Rb在Ser780位点磷酸化。PD 0332991(150 mg/kg)处理Colo-205 移植瘤,下调四种E2F调节的基因CDC2, CCNE2, TK1, 和 TOP2A表达。[1]PD 0332991也快速抑制骨髓瘤生长。[2]
动物实验 Animal Models 人类结肠癌移植瘤Colo-205
Dosages 150 mg/kg
Administration 每天口服处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05709158 Not yet recruiting
Breast Cancer
Pfizer
March 1 2024 --
NCT05912933 Not yet recruiting
Breast Cancer
Pfizer
March 1 2024 --
NCT05665361 Recruiting
Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc)
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
January 12 2024 Phase 1|Phase 2
NCT06076772 Not yet recruiting
Metastatic Breast Cancer
Assiut University
November 2023 --
NCT05655598 Recruiting
Advanced Breast Cancer|Treatment-Refractory Solid Tumors|Retinoblastoma Deficiency|SCLC|Soft Tissue Sarcoma|Endometrial Cancer|Bladder Cancer
Brown University
September 12 2023 Phase 1

化学信息&溶解度

分子量 573.66 分子式

C24H29N7O2.C2H6O4S

CAS号 827022-33-3 SDF Download Palbociclib Isethionate SDF
Smiles CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O
储存条件(自收到货起)

体外溶解度
批次:

Water : 100 mg/mL

DMSO : Insoluble ( DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
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

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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,: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: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: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:
What is the best vehicle for palbociclib for in vitro and in vivo?

回答:
You can use water for vitro use and Saline for vivo use.

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