PND-1186 hydrochloride (VS-4718 hydrochloride) 是一种有效的，高特异性的，可逆的 FAK 抑制剂，IC50 为 1.5 nM。PND-1186 hydrochloride 选择性促进肿瘤细胞凋亡 (apoptosis)。
货号:ajcx33074
CAS:1356154-94-3
分子式:C25H27ClF3N5O3
分子量：537.96
溶解度:DMSO : 200 mg/mL (371.77 mM; Need ultrasonic)|H2O : 20 mg/mL (37.18 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis[1].

PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397[1]. In murine 4T1 breast carcinoma cells, FAK is important in promoting an invasive and metastatic cell phenotype. Increasing concentrations of PND-1186 (0.1 to 1.0 µM) added to 4T1 cells inhibits FAK Tyr-397 phosphorylation (pY397) and results in elevated levels of total FAK protein within 1 h[1].

PND-1186 (30 mg/kg or 100 mg/kg; subcutaneously; injected subcutaneously in the neck region) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis[1].

[1]. Tanjoni I, et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.