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VER-50589

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Chemical Structure| 747413-08-7 同义名 : -
CAS号 : 747413-08-7
货号 : A922584
分子式 : C19H17ClN2O5
纯度 : 99%+
分子量 : 388.802
MDL号 : MFCD18382095
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.6 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：
生物活性
描述 VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM. It effectively blocks the intrinsic ATPase activity of recombinant yeast Hsp90 with an IC50 of 143 ± 23 nM in the presence of 400 μM ATP. This compound has demonstrated anti-proliferative effects across a range of human cancer cell lines, including a notably low GI50 of 32.7 ± 0.2 nM in CH1 human ovarian cells, and an average GI50 of 78 ± 15 nM. It also inhibits the proliferation of human umbilical vein endothelial cells (HUVEC) with a GI50 of 19 ± 2.4 nM, while exhibiting higher GI50 values in non-tumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. The cellular activities of VER-50589, which include causing cell cycle arrest and cytostasis in HCT116 colon cancer cells, do not depend on NQO1 expression and have been observed to lead to significant drug accumulation in these cells[1].
作用机制 The isoxazole VER-50589 makes essentially identical interactions in the ATP-binding site of human HSP90α.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.72mL

5.14mL

2.57mL
参考文献

[1]Sharp SY, 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.