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CAS No.: 747413-08-7

VER-50589 Catalog No. CSN13596

Synonyms: Ver-50589

VER-50589 is an isoxazole compound that inhibits Hsp90 with an IC50 value of 21 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述VER-50589 is an Hsp90 inhibitor with IC50 value of 21nM in a competitive binding assay. VER-50589 exhibited antiproliferation on a human cancer cell line panel, across melanoma, colon cancer, ovarian cancer and breast cancer, with GI50 values ranging in 78-685nM. Consistent with HSP90 inhibition, VER-50589 caused induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5, in SKMEL 2 human melanoma cells (310nM) and BT20 human breast cancer cells (247nM) post time>16h. It caused both cell cycle arrest and apoptosis. Administration of VER-50589 at dose of 100mg/kg, i.p., daily for 9 days, accumulated in HCT116 human colon cancer xenografts at levels above the cellular GI50 for 24 h, resulting in 30% growth inhibition.
作用机制The isoxazole VER-50589 makes essentially identical interactions in the ATP-binding site of human HSP90α.
参考文献

[1] Gaspar N, Sharp SY, et al. Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG,tanespimycin) in glioblastoma cells. Cancer Res. 2009 Mar 1;69(5):1966-75.
[2] Sharp SY, Prodromou C, et al. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther. 2007 Apr;6(4):1198-211.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5720 mL
- 12.8600 mL
- 25.7201 mL
- 5 mM
- 0.5144 mL
- 2.5720 mL
- 5.1440 mL
- 10 mM
- 0.2572 mL
- 1.2860 mL
- 2.5720 mL

技术信息

CAS号

747413-08-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17ClN2O5

运输

蓝冰

分子量

388.80

别名

Ver-50589

溶解度

DMSO	77.0 mg/mL (198.0 mM)
Water	Insoluble
Ethanol	77.0 mg/mL (198.0 mM)

动物实验配方

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