- ￥179 - 4102
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- A922584
- 2026年05月29日
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- 详细信息
- 文献和实验
- 技术资料
- 英文名：
5-(5-Chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)isoxazole-3-carboxamide
- 供应商：
上海安毕达生物科技有限公司
- CAS号：
747413-08-7
- 规格：
50μL/1mL/1mg/5mg/10mg/50mg
| 规格： | 50μL | 产品价格： | ￥179.0 |
|---|---|---|---|
| 规格： | 1mL | 产品价格： | ￥1147.0 |
| 规格： | 1mg | 产品价格： | ￥308.0 |
| 规格： | 5mg | 产品价格： | ￥1043.0 |
| 规格： | 10mg | 产品价格： | ￥1736.0 |
| 规格： | 50mg | 产品价格： | ￥4102.0 |
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 cells1.
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 cells1.
In vivo, VER-50589 administered at 4 mg/kg intraperitoneally achieves complete HSP90 inhibition in mice with OVCAR3 human ovarian ascites tumors, and at 100 mg/kg, it significantly reduces tumor volume and weight in HCT116 colon carcinoma xenografts compared to control mice1.
In vivo, VER-50589 administered at 4 mg/kg intraperitoneally achieves complete HSP90 inhibition in mice with OVCAR3 human ovarian ascites tumors, and at 100 mg/kg, it significantly reduces tumor volume and weight in HCT116 colon carcinoma xenografts compared to control mice1.
溶解方案(细胞实验)
DMSO 中的溶解度 : ≥ 48 mg/mL (123.46 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|* "≥" means soluble, but saturation unknown.
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in the stir bar. 13.Bring the vlume up t 1 liter by adding mre f the Lysis buffer. 14.Add Tritn-X100 t a final cncentratin f 2% by vlume. Nte: The Tritn-X-100 will nt disslve immediately.It will g int slutin slwly ver night. 15.Stir gently ver night
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