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

Chemical Structure : Onalespib

CAS No.: 912999-49-6

Onalespib (AT13387, AT-13387)

货号: PC-25124Not For Human Use, Lab Use Only.

Onalespib (AT13387) is a highly potent HSP90 inhibitor with Ki of 0.71 nM by binding in the ATPase site at the N-terminus of Hsp90, inhibits HCT116 cell proliferation with IC50 of 48 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Onalespib (AT13387) is a highly potent HSP90 inhibitor with Ki of 0.71 nM by binding in the ATPase site at the N-terminus of Hsp90, inhibits HCT116 cell proliferation with IC50 of 48 nM.
Onalespib (AT13387) potently inhibits the expression of the oncogenic client proteins Raf-1 and CDK4 at 30 nM in the HCT116 cell line.
Onalespib (AT13387) potently inhibits the proliferation of a panel of human tumor cell lines (well over 100 cell lines have been tested), showing IC50 < 100 nM.
Onalespib (AT13387) (60 mg/kg ip 3 days on and 3 days off for four cycles) exhibits in vivo antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts.

物理化学性质&存储条件

分子量 409.53
分子式 C24H31N3O3
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

(2,4-Dihydroxy-5-isopropylphenyl)(5-((4-methylpiperazin-1-yl)methyl)isoindolin-2-yl)methanone

参考文献

1. Woodhead AJ, et al. J Med Chem. 2010 Aug 26;53(16):5956-69.

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