| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S81884-5mg |
99.0% | ￥650.00 | 9 | - | - | - |
|
S81884-10mg |
99.0% | ￥1000.00 | 9 | - | - | - |
|
S81884-50mg |
99.0% | ￥2400.00 | 2 | - | - | - |
|
S81884-100mg |
≥99% | ￥3400.00 | 货期：2-3天 | - | - | - |
|
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
| 产品描述： | Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. | ||||||||||||||||||||
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| 靶点： | FAK | ||||||||||||||||||||
| 体外研究： | Defactinib inhibits pFAK expression within 3 hours, with a gradual return of expression by 48 hours. Defactinib inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. Defactinib reduces levels of AKT and YB-1 in taxane-resistant cell lines. The expression of pFAK (Tyr397) is statistically significantly inhibited by Defactinib in a dose-dependent manner in all cell lines.Defactinib inhibits pFAK (Tyr397) expression within 3 hours, with a gradual return of expression by 48 hours | ||||||||||||||||||||
| 体内研究： | There is an 87.4% reduction in tumor weight by PTX monotherapy in the HeyA8 model, and combination therapy resulted in the greatest tumor weight reduction, with a 97.9% reduction (P=0.05 compared with PTX). Defactinib (25 mg/kg; twice a day or greater statistically; 3 hours) treatment significantly inhibits pFAK (Tyr397), with return of expression noted by 24 hours. Therefore, administration of Defactinib at 25 mg/kg twice a day is selected as the dosing schedule for subsequent therapy experiments. For therapy experiments, female nude mice bearing HeyA8 tumors in the peritoneal cavity are randomly divided into 4 groups (n=10 per group): 1) vehicle orally twice daily and phosphate-buffered saline intraperitoneally weekly (control); 2) Defactinib 25 mg/kg orally twice daily; 3) PTX intraperitoneally weekly; and 4) both VDefactinib 25 mg/kg orally twice daily and PTX intraperitoneally weekly. In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001). | ||||||||||||||||||||
| 参考文献： | 1. Kang Y, et al. Role of focal adhesion kinase in regulating YB-1-mediated resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95. | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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