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Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。

PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC 50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis [1].

PND-1186 has an IC 50 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]. Western Blot Analysis [1] Cell Line: 4T1 breast carcinoma cells Concentration: 0.1, 0.2, 0.4, 0.6 and 1.0 μM Incubation Time: 1 hour Result: Inhibited FAK Tyr-397 phosphorylation (pY397) and resulted in elevated levels of total FAK protein.

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]. Animal Model: BALB/c mice [1] Dosage: 30 mg/kg or 100 mg/kg Administration: Injected (100 μL) subcutaneously in the neck region; every 12 h (twice-daily, b.i.d.) for 5 days. Result: 100 mg/kg treatment significantly reduced final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly reduced final tumor weight but was not significantly different compared to control.

1356154-94-3

C25H27ClF3N5O3

537.96

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years