PND-1186

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PND-1186 (VS-4718) 是一种可逆的选择性 FAK 抑制剂，IC50 为 1.5 nM。阶段1。

PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.(In Vitro):PND-1186 has an IC50 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.(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.

PND-1186 has an IC50 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. Western Blot Analysis 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. Animal Model:BALB/c miceDosage: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.

SR 2516 | VS-4718

Tyrosine Kinase

FAK

FAK

Cancer

——

1061353-68-1

501.5

C25H26F3N5O3

>98% (HPLC)

DMSO: 24 mg/mL (47.85 mM)

O=C(NC)C1=CC=CC=C1NC2=CC(NC3=C(OC)C=C(N4CCOCC4)C=C3)=NC=C2C(F)(F)F

2-((2-((2-methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide.

(-20℃)

With Ice Pack

≥ 2 years