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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-STA-9090
STA-9090

Chemical Structure : STA-9090

CAS No.: 888216-25-9

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STA-9090 (Ganetespib, STA9090)

货号: PC-20710Not For Human Use, Lab Use Only.

Ganetespib (STA 9090) is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).

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25 mg ￥1280 In stock
100 mg ￥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ganetespib (STA 9090) is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).
Ganetespib blocks the ability of HSP90 to bind to biotinylated geldanamycin and disrupts the association of HSP90 with its cochaperone, p23, more potently than 17-AAG.
Ganetespib causes depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC50 of 2-30 nM, in NSCLC cell lines.
Ganetespib is also approximately 20-fold more potent than 17-AAG in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants.
Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and acts as a potent Hsp90 inhibitor by inducing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2, c-Met, and Wilms' tumor 1.

物理化学性质&存储条件

分子量 364.41
分子式 C20H20N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one

参考文献

1. Lin TY, et al. Exp Hematol. 2008 Oct;36(10):1266-77.

2. McCleese JK, et al. Int J Cancer. 2009 Dec 15;125(12):2792-801.

3. Bansal H, et al. Blood. 2010 Nov 25;116(22):4591-9.

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