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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. In Vitro PND-1186 has an IC 50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c mice 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. Form:Solid
中文名称
PND-1186 hydrochloride
英文名称
PND-1186 hydrochloride
中文别名
PND-1186 盐酸盐
英文别名
UNII-S803K9N9TL | 2-(2-(2-Methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridine-4-ylamino)-N-methylbenzamide hydrochloride | S803K9N9TL | SR-2516 (hydrochloride) | VS-4718 hydrochloride | PND-1186 hydrochloride | MS-29927 | HY-13917A | Benzamide, 2
CAS号
1356154-94-3
分子式
C25H27ClF3N5O3
分子量
537.96 g/mol
精确质量
≥98%
PSA
87.800 Ų
Logp
-
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PND-1186 hydrochloride 10mM in DMSO 1ml

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