貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S81884-5mg	99.0%	￥650.00 S81884-5mg ￥650.00 現(xiàn)貨	9 9	-	-	-
S81884-10mg	99.0%	￥1000.00 S81884-10mg ￥1000.00 現(xiàn)貨	9 9	-	-	-
S81884-50mg	99.0%	￥2400.00 S81884-50mg ￥2400.00 現(xiàn)貨	2 2	-	-	-
S81884-100mg	≥99%	￥3400.00 S81884-100mg ￥3400.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

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.

產(chǎn)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.

靶點(diǎn)：

FAK

體外研究：

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

體內(nèi)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).

參考文獻(xiàn)：

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

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.828 ml	9.142 ml	18.283 ml
5 mM	0.366 ml	1.828 ml	3.657 ml
10 mM	0.183 ml	0.914 ml	1.828 ml
50 mM	0.037 ml	0.183 ml	0.366 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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Defactinib (hydrochloride)