Ganetespib | STA-9090 | HSP90 Inhibitor | AmBeed-信号通路专用抑制剂

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Ganetespib {[allProObj[0].p_purity_real_show]}

货号：A156855 同义名： STA-9090

Ganetespib (STA-9090) 是一种 HSP90 抑制剂，在各种血液和实体瘤细胞系中表现出强效细胞毒性。它还通过抑制 HIF-1α 和 STAT3 在结直肠癌中表现出抗血管生成作用。

Ganetespib 化学结构
CAS号：888216-25-9

Ganetespib 3D分子结构
CAS号：888216-25-9

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Ganetespib 纯度/质量文件产品仅供科研

货号：A156855 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

Ganetespib 生物活性

描述

HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. Ganetespib is a novel HSP90 inhibitor which is a resorcinol-containing triazole compound unrelated to the first class of HSP90 inhibitors, geldanamycin, 17-AAG and 17-DMAG. As both AKT and KIT are the client protein of HSP90 and are stabilized by it, inhibition of HSP90 by 100nM Ganetespib for 24h caused downregulation of both KIT and AKT only on protein level in BR can C2 cells, as well as a disruption of the association of HSP90 with Kit. Meanwhile, as upregulation of HSP70 is a consequence of HSP90 inhibition, exposure to Ganetespib also caused an induction of HSP70 expression in cells. STA-9090 led to 72-hour growth inhibition of malignant canine mast cell lines C2 and BR with IC50 values of 19nM and 4nM, respectively, much lower than 17-AAG (IC50=948nm (C2) and 44 nm (BR)). Treatment with Ganetespib caused cell apoptosis, shown as increased Annexin V-phycoerythrin [PE] /7-amino-actinomycin D (7-AAD) and increased Sub-G1 level in C2, BR, and BMCMC treated with 100nM Ganetespib for 24 or 48h, cleaved PARP induced by 100 or 1000nM Ganetespib for 24h in BR and C2 cells, and increased caspase3/7 in C2 cells treated with 50 or 75nM Ganetespib for 24h. Intravenous injection with Ganetespib at concentration of 25mg/kg, 3 days on and 2 days off, for 17 days significantly inhibited tumor growth in the C2 xenograft model^[1].

作用机制

Ganetespib can bind in the ATP-binding domain at the N-terminus of HSP90. ^[1]

Ganetespib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
35612		Growth Inhibition Assay		IC50=38 nM	24784839
5637		Growth Inhibition Assay		IC50=44 nM	24784839
639-V		Growth Inhibition Assay		IC50=10 nM	24784839
647-V		Growth Inhibition Assay		IC50=27 nM	24784839

Ganetespib 动物研究

Dose

Mice (i.v.): min = 25 mg/kg^[2], max = 100 mg/kg^[3] (i.v.)

Administration

i.v.

Pharmacokinetics

Animal	Rats^[4]
Dose	20 mg/kg
Administration	i.v.
T_1/2	6.4 h
T_max	0.083 h
C_max	110 μM
AUC	36.1 μM·h

Ganetespib 参考文献

[1]Lin TY, Bear M, et al. The novel HSP90 inhibitor STA-9090 exhibits activity against Kit-dependent and -independent malignant mast cell tumors. Exp Hematol. 2008;36(10):1266-77.

[2]Shimamura T, Perera SA, et al. Ganetespib (STA-9090), a nongeldanamycin HSP90 inhibitor, has potent antitumor activity in in vitro and in vivo models of non-small cell lung cancer. Clin Cancer Res. 2012 Sep 15;18(18):4973-85.

[3]Nagaraju GP, Mezina A, et al. Targeting the Janus-activated kinase-2-STAT3 signalling pathway in pancreatic cancer using the HSP90 inhibitor ganetespib. Eur J Cancer. 2016 Jan;52:109-19.

[4]Zhou D, Liu Y, et al. A rat retinal damage model predicts for potential clinical visual disturbances induced by Hsp90 inhibitors. Toxicol Appl Pharmacol. 2013 Dec 1;273(2):401-9.

Ganetespib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL

Ganetespib 技术信息

CAS号	888216-25-9
分子式	C₂₀H₂₀N₄O₃
分子量	364.398

别名	STA-9090
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(288.15 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 4.4 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

35612		Growth Inhibition Assay		IC50=38 nM	24784839
5637		Growth Inhibition Assay		IC50=44 nM	24784839
639-V		Growth Inhibition Assay		IC50=10 nM	24784839
647-V		Growth Inhibition Assay		IC50=27 nM	24784839
A1847	0-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	23900136
A1847	10-100 nM	Apoptosis Assay	24/48/72 h	induces apoptosis time and dose dependently	23900136
A549		Growth Inhibition Assay		IC50=43 nM	23012248
AC3		Growth Inhibition Assay		IC50=25.9 nM	24166505
BFTC		Growth Inhibition Assay		IC50=17 nM	24784839
BT-12		Growth Inhibition Assay		IC50=14.3 nM	23303741
BT-20	100/250 nM	Function Assay	24 h	resulted in a dose-dependent destabilization of EGFR, IGF-IR, MET, and CRAF	24173541
CAL27	10/50 nM	Cytoxicity Assay	24 h	decreases cell proliferation dose dependently	25205430
Calu-1		Growth Inhibition Assay		IC50=58 nM	23012248
Calu-6		Growth Inhibition Assay		IC50=64 nM	23012248
CCRF-CEM (1)		Growth Inhibition Assay		IC50=12.5 nM	23303741
CCRF-CEM (2)		Growth Inhibition Assay		IC50=7.2 nM	23303741
CHLA-10		Growth Inhibition Assay		IC50=5.7 nM	23303741
CHLA-136		Growth Inhibition Assay		IC50=23.2 nM	23303741
CHLA-258		Growth Inhibition Assay		IC50=6.4 nM	23303741
CHLA-266		Growth Inhibition Assay		IC50=27.1 nM	23303741
CHLA-9		Growth Inhibition Assay		IC50=4.6 nM	23303741
CHLA-90		Growth Inhibition Assay		IC50=22.3 nM	23303741
COG-LL-317		Growth Inhibition Assay		IC50=4.4 nM	23303741
COLO-205		Growth Inhibition Assay		IC50=14 nM	24682747
COLO-678		Growth Inhibition Assay		IC50=21 nM	24682747
COR-L23		Growth Inhibition Assay		IC50=22 nM	23012248
Detroit562	10/50 nM	Cytoxicity Assay	24 h	decreases cell proliferation dose dependently	25205430
DSH1		Growth Inhibition Assay		IC50=6 nM	24784839
FUDA	10/50 nM	Cytoxicity Assay	24 h	decreases cell proliferation dose dependently	25205430
GLC4		Growth Inhibition Assay		IC50=20.47 nM	24166505
GLC4	30 nM	Function Assay	72 h	induces persistent G2/M phase arrest	24166505
H1173		Growth Inhibition Assay		IC50=12.62 nM	24166505
H128		Growth Inhibition Assay		IC50=69.55 nM	24166505
H1355		Growth Inhibition Assay		IC50=5 nM	23012248
H146		Growth Inhibition Assay		IC50=28.51 nM	24166505
H146	30 nM	Function Assay	72 h	induces persistent G2/M phase arrest	24166505
H157		Growth Inhibition Assay		IC50=7 nM	23012248
H1734		Growth Inhibition Assay		IC50=28 nM	23012248
H1792		Growth Inhibition Assay		IC50=20 nM	23012248
H187		Growth Inhibition Assay		IC50=24.99 nM	24166505
H2009		Growth Inhibition Assay		IC50=19 nM	23012248
H2030		Growth Inhibition Assay		IC50=12 nM	23012248
H2122		Growth Inhibition Assay		IC50=53 nM	23012248
H2212		Growth Inhibition Assay		IC50=17 nM	23012248
H2228	0-1000 nM	Cell Viability Assay	72 h	IC50=13 nM	23533265
H23		Growth Inhibition Assay		IC50=11 nM	23012248
H3122	0-1000 nM	Cell Viability Assay	72 h	IC50=10 nM	23533265
H358		Growth Inhibition Assay		IC50=29 nM	23012248
H441		Growth Inhibition Assay		IC50=14 nM	23012248
H460		Growth Inhibition Assay		IC50=8 nM	23012248
H526		Growth Inhibition Assay		IC50=21.64 nM	24166505
H620		Growth Inhibition Assay		IC50=32.67 nM	24166505
H69		Growth Inhibition Assay		IC50=83.36 nM	24166505
H727		Growth Inhibition Assay		IC50=28 nM	23012248
H792		Growth Inhibition Assay		IC50=45.07 nM	24166505
H82		Growth Inhibition Assay		IC50=30.27 nM	24166505
H82	30 nM	Function Assay	72 h	induces persistent G2/M phase arrest	24166505
HCC2998		Growth Inhibition Assay		IC50=128 nM	24682747
HCT 116		Growth Inhibition Assay		IC50=14 nM	24682747
HCT-116	50nM	Function Assay	24 h	induced G0/G1 arrest	25210794
HCT-15		Growth Inhibition Assay		IC50=8 nM	24682747
HL60	30/80/150/250 nM	Apoptosis Assay	24/48/72 h	induces dose dependant induction of apoptosis	25882550
HOP-62		Growth Inhibition Assay		IC50=11 nM	23012248
HT-1197		Growth Inhibition Assay		IC50=53 nM	24784839
HT-1376		Growth Inhibition Assay		IC50=21 nM	24784839
HT-29	50nM	Function Assay	24 h	induced G0/G1 arrest	25210794
HuTu-80		Growth Inhibition Assay		IC50=13 nM	24682747
IA-LM		Growth Inhibition Assay		IC50=10 nM	23012248
J82		Growth Inhibition Assay		IC50=18 nM	24784839
K008		Cell Viability Assay		IC50=60 nM	23418523
K008	250 nM	Function Assay	24 h	induces G2 arrest	23418523
K008	100 nM	Apoptosis Assay	72 h	significantly induces apoptosis	23418523
K028		Cell Viability Assay		IC50=84 nM	23418523
K028	250 nM	Function Assay	24 h	induces G2 arrest	23418523
K028	100 nM	Apoptosis Assay	72 h	significantly induces apoptosis	23418523
K029		Cell Viability Assay		IC50=46 nM	23418523
K029	250 nM	Function Assay	24 h	induces G1 arrest	23418523
K029	100 nM	Apoptosis Assay	72 h	significantly induces apoptosis	23418523
K033		Cell Viability Assay		IC50=75.5 nM	23418523
K033	250 nM	Function Assay	24 h	induces a modest increase in G1 population	23418523
K033	100 nM	Apoptosis Assay	72 h	significantly induces apoptosis	23418523
Karpas-299		Growth Inhibition Assay		IC50=9.6 nM	23303741
Kasumi-1		Growth Inhibition Assay		IC50=5.8 nM	23303741
KU-19-19		Growth Inhibition Assay		IC50=36 nM	24784839
LB831-BLC		Growth Inhibition Assay		IC50=34 nM	24784839
LNCaP		Growth Inhibition Assay		IC50=8 nM	23152004
LoVo		Growth Inhibition Assay		IC50=22 nM	24682747
LS-1034		Growth Inhibition Assay		IC50=31 nM	24682747
LS-123		Growth Inhibition Assay		IC50=73 nM	24682747
LS-411 N		Growth Inhibition Assay		IC50=5 nM	24682747
M23		Cell Viability Assay		IC50=37.5 nM	23418523
M23	250 nM	Function Assay	24 h	induces G1 and G2/M arrest	23418523
M23	100 nM	Apoptosis Assay	72 h	significantly induces apoptosis	23418523
MDA-MB-231	100 nM	Function Assay	30 min	inhibits accumulation of HIF-1α	24248265
MDA-MB-231	100 nM	Function Assay	24 h	inhibits the migratory and invasive capacity	24173541
MDA-MB-435	100 nM	Function Assay	30 min	inhibits accumulation of HIF-1α	24248265
MGC-803	0.1-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25590805
MGC-803	0.1-1000 nM	Function Assay	24 h	induces G2/M cell-cycle arrest	25590805
MGH-U3		Growth Inhibition Assay		IC50=53 nM	24784839
MKN-28	0.1-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25590805
MOLT-4		Growth Inhibition Assay		IC50=10.6 nM	23303741
MV411	30/80/150/250 nM	Apoptosis Assay	24/48/72 h	induces dose dependant induction of apoptosis	25882550
N592		Growth Inhibition Assay		IC50=14.12 nM	24166505
NALM-6		Growth Inhibition Assay		IC50=11.7 nM	23303741
NB-1643		Growth Inhibition Assay		IC50=7.4 nM	23303741
NB-EBc1		Growth Inhibition Assay		IC50=16.8 nM	23303741
NCI-H1975		Growth Inhibition Assay	48 h	IC50=16 nM	22144665
NCI-H1975		Growth Inhibition Assay	72 h	IC50=8 nM	22144665
NCI-H747		Growth Inhibition Assay		IC50=17 nM	24682747
OVCAR-5	0-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	23900136
OVCAR-5	10-100 nM	Apoptosis Assay	24/48/72 h	induces apoptosis time and dose dependently	23900136
OVCAR-8	0-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	23900136
OVCAR-8	10-100 nM	Apoptosis Assay	24/48/72 h	induces apoptosis time and dose dependently	23900136
Ramos-RA1		Growth Inhibition Assay		IC50=7.4 nM	23303741
RD		Growth Inhibition Assay		IC50=8 nM	23303741
Rh18		Growth Inhibition Assay		IC50=6.2 nM	23303741
Rh30		Growth Inhibition Assay		IC50=5.6 nM	23303741
Rh41		Growth Inhibition Assay		IC50=10.4 nM	23303741
RKO		Growth Inhibition Assay		IC50=4 nM	24682747
RS4;11		Growth Inhibition Assay		IC50=13.5 nM	23303741
RT112		Growth Inhibition Assay		IC50=9 nM	24784839
RT4		Growth Inhibition Assay		IC50=1733 nM	24784839
SCaBER		Growth Inhibition Assay		IC50=10 nM	24784839
SCC25	10/50 nM	Cytoxicity Assay	24 h	decreases cell proliferation dose dependently	25205430
SGC-7901	0.1-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25590805
SJ-GBM2		Growth Inhibition Assay		IC50=12.9 nM	23303741
SK-CO-1		Growth Inhibition Assay		IC50=81 nM	24682747
SK-LU-1		Growth Inhibition Assay		IC50=18 nM	23012248
SKOV-3	0-1000 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	23900136
SNU-C2B		Growth Inhibition Assay		IC50=45 nM	24682747
SW-1710		Growth Inhibition Assay		IC50=6 nM	24784839
SW620		Growth Inhibition Assay		IC50=8 nM	24682747
SW780		Growth Inhibition Assay		IC50=3451 nM	24784839
T24		Growth Inhibition Assay		IC50=7 nM	24784839
TC-71		Growth Inhibition Assay		IC50=4.5 nM	23303741
TCCSUP		Growth Inhibition Assay		IC50=142 nM	24784839
UM-UC3		Growth Inhibition Assay		IC50=33 nM	24784839
VCaP		Growth Inhibition Assay		IC50=7 nM	23152004

Ganetespib {[allProObj[0].p_purity_real_show]}

Ganetespib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Ganetespib 质控信息

Ganetespib 生物活性

Ganetespib 细胞研究

Ganetespib 动物研究

Ganetespib 参考文献

Ganetespib 实验方案

Ganetespib 技术信息

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Ganetespib {[allProObj[0].p_purity_real_show]}

Ganetespib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Ganetespib 质控信息

Ganetespib 生物活性

Ganetespib 细胞研究

Ganetespib 动物研究

Ganetespib 参考文献

Ganetespib 实验方案

Ganetespib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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