Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 397 | 5日内发货 | ||
5 mg | ¥ 663 | 5日内发货 | ||
10 mg | ¥ 990 | 5日内发货 | ||
25 mg | ¥ 1,920 | 5日内发货 |
Defactinib hydrochloride 的其他形式现货产品:
产品描述 | Defactinib hydrochloride (PF 04554878 hydrochloride) is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. |
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]. |
别名 | VS-6063 hydrochloride, PF 04554878 hydrochloride |
分子量 | 546.95 |
分子式 | C20H22ClF3N8O3S |
CAS No. | 1073160-26-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (41.1 mM), Sonification is recommended.
H2O: 0.1 mg/mL (insoluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8283 mL | 9.1416 mL | 18.2832 mL | 45.708 mL |
5 mM | 0.3657 mL | 1.8283 mL | 3.6566 mL | 9.1416 mL | |
10 mM | 0.1828 mL | 0.9142 mL | 1.8283 mL | 4.5708 mL | |
20 mM | 0.0914 mL | 0.4571 mL | 0.9142 mL | 2.2854 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Defactinib hydrochloride 1073160-26-5 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK VS-6063 hydrochloride PF 04554878 hydrochloride PF04554878 Hydrochloride VS-6063 Hydrochloride VS6063 Hydrochloride PF-04554878 Hydrochloride Defactinib Hydrochloride PF 04554878 Hydrochloride VS 6063 Hydrochloride Inhibitor inhibitor inhibit