地法替尼盐酸盐 T15092

Product Introduction
Bioactivity


英文名: Defactinib hydrochloride

描述: Defactinib hydrochloride (PF 04554878 hydrochloride) (VS-6063 hydrochloride; PF 04554878 hydrochloride) 是一种新型 FAK 抑制剂，抑制 FAK 在 Tyr397 位点磷酸化，这种作用具有时间和剂量依赖性。

体外活性: 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. RPPA data displays that 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 [1].

体内活性: 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)[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 22.5 mg/mL (41.1 mM)
H2O : 0.1 mg/mL (insoluble)


关键字: PF04554878 Hydrochloride | VS-6063 Hydrochloride | VS6063 Hydrochloride | PF-04554878 Hydrochloride | Defactinib Hydrochloride | PF 04554878 Hydrochloride | VS 6063 Hydrochloride

相关产品: ALK inhibitor 1 | PF-562271 hydrochloride | CEP-37440 | SU6656 | Excisanin A | 5α-Hydroxycostic acid | FAK-IN-11 | PND-1186 | Nitidine chloride | NVP-TAE 226

相关库: Anti-Ovarian Cancer Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途