Geldanamycin

别名: NSC 122750 中文名称：格尔德霉素

目录号：S2713 Purity: 99.84%

Geldanamycin是一种天然的HSP90抑制剂，K_d为1.2 μM，特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。

Geldanamycin Chemical Structure

CAS: 30562-34-6

规格	价格	库存
10mM (1mL in DMSO)	3131.63	现货
5mg	1407.44	现货
50mg	5493.81	现货
1g	32678.1	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： 99.84%

99.84

Geldanamycin相关产品

相关产品	Puromycin 2HCl Staurosporine (STS) Oligomycin A Honokiol Geneticin (G418 Sulfate) STZ (Streptozotocin) Cephalomannine Sodium Monensin (NSC 343257) 10-Deacetylbaccatin-III Pirarubicin Hygromycin B Roxithromycin	点击展开
相关化合物库	激酶抑制剂库血管生成相关化合物库 TGF-beta/Smad信号通路库细胞骨架信号通路化合物库抗心血管疾病化合物库	点击展开

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
rat neuronal cells	Cytotoxicity assay	10 uM	24 hrs	Cytotoxicity against rat neuronal cells at 10 uM after 24 hrs	17276679
PP30	Function assay	100 uM	3 hrs	Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as induction of heat shock response at 100 uM after 3 hrs	21129982
MCF7	Function assay	500 nM	24 hrs	Inhibition of Hsp90 in human MCF7 cells assessed as induction of Her2 degradation at 500 nM after 24 hrs by Western blot method	21861487
MCF7	Function assay	500 nM	24 hrs	Inhibition of Hsp90 in human MCF7 cells assessed as induction of Raf degradation at 500 nM after 24 hrs by Western blot method	21861487
MCF7	Function assay	500 nM	24 hrs	Inhibition of Hsp90 in human MCF7 cells assessed as induction of Akt degradation at 500 nM after 24 hrs by Western blot method	21861487
SKBR3	Function assay	0.5 uM	18 hrs	Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 0.5 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis	23859777
CL1-5	Function assay	2 uM	16 hrs	Inhibition of HSP90 in human CL1-5 cells assessed as reduction of total Akt at 2 uM after 16 hrs by Western blotting analysis	24428777
MDA-MB 231	Function assay	0.5 uM	24 hrs	Inhibition Hsp90 in human MDA-MB 231 cells assessed as increase in HSP70 protein level at 0.5 uM incubated for 24 hrs by Western blot method	25277067
PC12	Function assay	10 uM	3 to 16 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of intracellular D-aspartate content at 10 uM measured at 3 to 16 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis relative to vehicle-t	26642769
PC12	Function assay	10 uM	6 to 16 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of total D-aspartate content at 10 uM measured at 6 to 16 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis relative to vehicle-treated c	26642769
PC12	Function assay	up to 10 uM	24 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of D-aspartate level in cell culture medium up to 10 uM after 24 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis	26642769
A549	Function assay	5 to 10 uM	24 hrs	Inhibition of HSP90alpha in human A549 cells assessed as upregulation of HSP90alpha expression at 5 to 10 uM after 24 hrs by Western blot analysis	29486954
A549	Function assay	5 to 10 uM	24 hrs	Inhibition of HSP90beta in human A549 cells assessed as upregulation of HSP90beta expression at 5 to 10 uM after 24 hrs by Western blot analysis	29486954
Jurkat	Function assay	1 uM		Inhibition of to HSP90 in FADD deficient human Jurkat cells assessed as RIP protein degradation at 1 uM by Western blot	18408713
SK-BR-3	Function assay	50 mg/kg		Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose, IC50=0.07μM	7562911
SH-SY5Y	Neuroprotection assay	10 nM		Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM	19138859
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Akt degradation at 0.5 uM by Western blot analysis	21273068
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Raf degradation at 0.5 uM by Western blot analysis	21273068
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Hsp90 degradation at 0.5 uM by Western blot analysis	21273068
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Her2 degradation at 0.5 uM by Western blot analysis	21273068
MDA-MB 231	Function assay	0.5 and 5 uM		Inhibition of HSP90 in human MDA-MB 231 cells assessed increase in HSP70 protein levels at 0.5 and 5 uM by Western blot method	25105924
KPL4	Function assay		40 hrs	Inhibition of Hsp90 in human KPL4 cells assessed as depletion of Raf-1 level after 40 hrs, MEC=0.33μM	18243703
KPL4	Function assay		40 hrs	Inhibition of Hsp90 in human KPL4 cells assessed as depletion of ErbB2 level after 40 hrs, MEC=0.11μM	18243703
P19	Cytotoxicity assay		18 hrs	Cytotoxicity against mouse P19 cells after 18 hrs, IC50=0.1μM	17442565
SKBR3	Function assay		24 hrs	Inhibition of Hsp90-mediated HER2 degradation in human SKBR3 cells after 24 hrs by Western blot	18816111
SKBR3	Function assay		24 hrs	Inhibition of Hsp90-mediated Raf degradation in human SKBR3 cells after 24 hrs by Western blot	18816111
HuH7	Antiviral assay		3 days	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis, EC50=0.00025μM	18936191
HuH7	Antiviral assay		3 days	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis, EC50=0.0012μM	18936191
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay, IC50=0.041μM	19405528
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells after 72 hrs, IC50=0.2μM	20655237
HCT116	Antiproliferative assay		4 days	Antiproliferative activity against human HCT116 cells measured on day 4 by Cell titer-glo assay, EC50=0.03μM	21420297
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells at 72 hrs by MTS assay, IC50=0.053μM	22162786
SKBR3	Antiproliferative assay		72 hrs	Antiproliferative activity against estrogen receptor deficient human SKBR3 cells after 72 hrs, IC50=0.0085μM	23648180
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs, IC50=0.0098μM	23648180
A549	Cytotoxicity assay		2 days	Cytotoxicity against human A549 cells after 2 days by AlamarBlue assay, IC50=0.15μM	23947794
L6	Cytotoxicity assay		72 hrs	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay, IC50=6μM	24580531
Sf9	Function assay		16 hrs	Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay, IC50=0.074μM	24751441
MDA-kb2	Function assay		18 hrs	Inhibition of HSP90 in human MDA-kb2 cells assessed as reduction in glucocorticoid receptor-dependent luciferase expression after 18 hrs by firefly luciferase reporter gene assay, IC50<0.01μM	24984936
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.04μM	25075762
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.05μM	25105924
LNCAP	Cytotoxicity assay		72 hrs	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay, IC50=0.43μM	25105924
HUVEC	Cytotoxicity assay		72 hrs	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay, IC50=0.019μM	25277067
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells after 72 hrs by MTT assay, IC50=0.04μM	25277067
BGC823	Cytotoxicity assay		72 hrs	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay, IC50=0.04μM	25277067
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=0.04μM	25277067
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.05μM	25277067
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.097μM	25277067
HL7702	Cytotoxicity assay		72 hrs	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay, IC50=0.141μM	25277067
SW480	Cytotoxicity assay		72 hrs	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay, IC50=0.31μM	25277067
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.798μM	25277067
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.0427μM	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as pAkt degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as Her2 degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as Cdk6 degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as Raf degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Change in Cdc37 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Change in p23 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP90 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP70 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP27 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control	25756299
PC12	Function assay		24 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of intracellular D-aspartate level up to 10 uM after 24 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis	26642769
A549	Function assay		12 to 24 hrs	Inhibition of Hsp90 in human A549 cells assessed as decrease in EGFR levels at five times IC50 value after 12 to 24 hrs by Western blot analysis	26745854
A549	Function assay		12 to 24 hrs	Inhibition of Hsp90 in human A549 cells assessed as decrease in Her2 levels at five times IC50 value after 12 to 24 hrs by Western blot analysis	26745854
A549	Function assay		12 to 24 hrs	Inhibition of Hsp90 in human A549 cells assessed as decrease in C-Raf levels at five times IC50 value after 12 to 24 hrs by Western blot analysis	26745854
BA/F3	Function assay		48 hrs	Inhibition of imatinib-resistant BCR-ABL T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=1μM	26844689
BA/F3	Function assay		48 hrs	Inhibition of imatinib-resistant BCR-ABL E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=1μM	26844689
BA/F3	Function assay		48 hrs	Inhibition of BCR-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=5μM	26844689
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTS/PMS assay, Activity=0.06μM	27003516
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50=0.03μM	27266997
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50=0.06μM	27266997
SNU638	Anticancer assay		72 hrs	Anticancer activity against human SNU638 cells measured after 72 hrs by SRB assay, IC50=0.03μM	27283788
Caki1	Anticancer assay		72 hrs	Anticancer activity against human Caki1 cells measured after 72 hrs by SRB assay, IC50=0.056μM	27283788
A549	Anticancer assay		72 hrs	Anticancer activity against human A549 cells measured after 72 hrs by SRB assay, IC50=0.109μM	27283788
MDA-MB-231	Anticancer assay		72 hrs	Anticancer activity against human MDA-MB-231 cells measured after 72 hrs by SRB assay, IC50=0.11μM	27283788
HCT116	Anticancer assay		72 hrs	Anticancer activity against human HCT116 cells measured after 72 hrs by SRB assay, IC50=0.15μM	27283788
SKBR3	Antiproliferative assay		1 to 3 days	Antiproliferative activity against Her2-overexpressing human SKBR3 cells after 1 to 3 days by MTS assay, GI50=0.43μM	27783977
NCI-H1975	Antiproliferative assay		1 to 3 days	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay, GI50=0.56μM	27783977
RPMI8226	Growth inhibition assay		72 hrs	Growth inhibition of human RPMI8226 cells after 72 hrs by MTS/PMS assay, GI50=0.003μM	29057043
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50=0.06μM	29172085
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50=0.1μM	29172085
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by Cell Titer 96 Aqueous One Solution cell proliferation assay, GI50=0.56μM	29202402
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of Raf1 protein degradation incubated for 24 hrs by Western blot analysis	31591016
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of CDK4 protein degradation incubated for 24 hrs by Western blot analysis	31591016
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of Her2 protein degradation incubated for 24 hrs by Western blot analysis	31591016
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of AKT protein degradation incubated for 24 hrs by Western blot analysis	31591016
Jurkat	Function assay			Inhibition of TNF-alpha-induced NF-kappaB activation expressed in FADD deficient human Jurkat cells by luciferase reporter gene assay	18408713
HEK293T	Function assay			Inhibition of TNF-alpha-induced NF-kappaB activation expressed in HEK293T cells by luciferase reporter gene assay	18408713
A549	Growth inhibition assay			Growth inhibition of human A549 cells, GI50=0.064μM	18243703
KPL4	Growth inhibition assay			Growth inhibition of human KPL4 cells, GI50=0.059μM	18243703
DLD1	Growth inhibition assay			Growth inhibition of human DLD1 cells, GI50=0.037μM	18243703
HCT116	Growth inhibition assay			Growth inhibition of human HCT116 cells, GI50=0.021μM	18243703
MCF7	Growth inhibition assay			Growth inhibition of human MCF7 cells after days by SRB assay, GI50=35.6μM	17869098
LS174T	Cytotoxicity assay			Cytotoxicity against human LS174T cells by MTS assay, IC50=0.45μM	17034135
HEK293	Function assay			Inhibition of HSP90 expressed in HEK293 cells assessed as effect on Akt1:p27 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay	16680159
SKBR-3	Function assay			Effective concentration for Her-2 degradation in SKBR-3 cells, Concentration=5μM	15713410
MCF-7	Function assay			Inhibition of steady-state expression of Raf-1 in MCF-7 breast cancer cells, IC50=0.2μM	10340605
MCF-7	Function assay			Inhibition of steady-state expression of ER in MCF-7 breast cancer cells, IC50=0.06μM	10340605
MCF-7	Function assay			Inhibition of steady-state expression of HER2 in MCF-7 breast cancer cells, IC50=0.05μM	10340605
SK-BR-3	Function assay			In vitro inhibition of p185 erbB-2 oncoprotein in human breast cancer SK-BR-3 cells, IC50=0.07μM	7562912
HT-29 cell	Growth inhibition assay			Inhibitory concentration against human colorectal carcinoma HT-29 cell lines, IC50=24.5 nM	15658879
K562 cell	Growth inhibition assay			Inhibitory concentration against human leukemia K562 cell lines, IC50=22.1 nM	15658879
MCF-7 cell	Growth inhibition assay			Inhibitory concentration against human breast cancer MCF-7 cell lines, IC50=6.5 nM	15658879
SW620 cell	Growth inhibition assay			Inhibitory concentration against human colorectal carcinoma SW620 cell lines, IC50=6.2 nM	15658879
A2780 cells	Proliferation assay			Compound was evaluated for antiproliferative activity against human ovarian carcinoma cell line A2780, IC50=3.4 μM	11514145
SH-SY5Y	Neuroprotection assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04269μM	19138859
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells by SRB assay, IC50=9.6μM	19560353
SK-BR-3	Antiproliferative assay			Antiproliferative activity against human SK-BR-3 cells, IC50=0.0158μM	19896848
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells, IC50=0.0161μM	19896848
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells by luminescence assay, EC50=0.03μM	21605975
U87	Antiproliferative assay			Antiproliferative activity against human U87 cells by luminescence assay, EC50=0.089μM	21605975
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells, IC50=0.03μM	21715165
NCI-H1975	Antiproliferative assay			Antiproliferative activity against human NCI-H1975 cells, IC50=0.036μM	21715165
U87MG	Antiproliferative assay			Antiproliferative activity against human U87MG cells, IC50=0.089μM	21715165
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, IC50=0.37μM	22849774
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells by MTT assay, IC50=0.3μM	23656556
SKBR3	Function assay			Inhibition of Hsp90 in human SKBR3 cells, IC50=0.07μM	26844689
点击查看更多细胞系数据

生物活性

产品描述

靶点

p185 ^[4] (SKBr3 cells)	HSP90 (N-terminal domain) ^[1] (Cell-free assay)	HSP90 ^[1] (Cell-free assay)
70 nM	0.78 μM(Kd)	1.2 μM(Kd)

体外研究(In Vitro)
体外研究活性	Geldanamycin结合于Hsp90s (残基1-220) N-末端结构域的ATP结合位点。Geldanamycin剂量依赖性抑制Hsp90的ATPase活性。^[1] 在A2780人卵巢细胞系中，Geldanamycin引起剂量依赖性G2期阻滞，并可逆抑制其进入S期。该抑制作用伴随p53的增加，最终证明是p53依赖性的。^[2] Geldanamycin引起p185受体蛋白-酪氨酸激酶的泛素化和蛋白酶体降解，IC50为70 nM。^{[3, 4]} Geldanamycin是典型的抗肿瘤试剂，对一组60个人肿瘤细胞系的平均GI50为0.18 μM。^[5]
激酶实验	核苷结合的等温滴定量热法(ITC)
激酶实验	滴定实验使用MSC系统进行。在每个实验中，16等份15 μL geldanamycin (300 μM在1% DMSO中)在25 °C下注射到1.3 mL蛋白质(31 μM在20 mMTris-HCl中, pH 7.5, 1 mMEDTA)，得到的数据减去稀释热后进行拟合。将geldanamycin加入缓冲液和缓冲液加入蛋白质的稀释热在单独实验中测定。在核苷酸结合位点没有观察到DMSO的结合。滴定数据使用非线性最小二乘法曲线拟合算法拟合，该算法有三个不固定变量：化学计量，结合常数(K_b) 1/K_d)，和相互作用焓的变化(ΔH°)。Geldanamycin结合到完整酵母Hsp90和Hsp90 N-末端结构域，估计的解离常数分别为1.22 μM和0.78 μM。结合到C-末端片段时，没有观察到有意义的热量。
细胞实验	细胞系	A2780人卵巢癌细胞系
	浓度	0.001-10 μM
	孵育时间	3小时
	方法	指数生长的细胞用Geldanamycin处理，不同时期的DNA合成通过溴脱氧尿苷(BrdUrd)的整合和流式细胞分析术评估。在此期间，处理的和未处理的细胞，总细胞数没有显著的差别。BrdUrd (10 μM)在37 °C下4小时的培育期间进行整合，将细胞采集并固定在70%乙醇中。DNA通过2 N HC1变性后，细胞用抗- BrdUrd小鼠单克隆抗体培育，随后用异硫氰酸荧光素(FITC)-连接的山羊抗-小鼠IgG培育。细胞在室温下用碘化丙啶着色30分钟，使用Coulter EPICS Profile分析器通过流式细胞术分析。

体内研究(In Vivo)
体内研究活性	在FRE/erbB-2 小鼠体内，Geldanamycin (50 mg//kg)对pl85-相关的磷酸酪氨酸水平表现出30%的抑制。^[6]
动物实验	Animal Models	负荷FRE/erbB-2肿瘤的nu/nu小鼠
	Dosages	50 mg/kg
	Administration	通过腹腔注射给药

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)
NCT00003969	Completed	Unspecified Adult Solid Tumor Protocol Specific	Cancer Research UK\|National Cancer Institute (NCI)	August 1998	Phase 1

参考文献
[1] Roe SM, et al, J Med Chem, 1999, 42(2), 260-266. [2] Mcllwrath AJ, et al, Cancer Chemother Pharmacol, 1996, 37(5), 423-428. [3] Mimnaugh EG, et al, J Biol Chem 1996, 271(37), 22796-22801. [4] Miller P, et al, Cancer Res, 1994, 54(10), 2724-2730. [5] Supko JG, et al, Cancer Chemother Pharmacol, 1995, 36(4), 305-315. [6] Schnur RC, et al. J Med Chem, 1995, 38(19), 3806-3812. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	560.64	分子式	C₂₉H₄₀N₂O₉
CAS号	30562-34-6	SDF	Download Geldanamycin SDF
Smiles	CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)C)OC)OC(=O)N)C)C)O)OC
储存条件(自收到货起)	3年-20°C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 : 33 mg/mL ( (58.86 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 : 50 mg/mL ( (89.18 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 : 100 mg/mL ( (178.36 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%PEG300 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。	1.650mg/ml (2.94mM)	以 1 mL 工作液为例,取50μL33mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 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。	0.410mg/ml (0.73mM)	以1 mL工作液为例，取50μL 8.2mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。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。

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。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

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):