产品
编 号：F024935
分子式：C25H26F3N5O3
分子量：501.5
分子式：C25H26F3N5O3
分子量：501.5
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1061353-68-1
产品详情
生物活性：
PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
体内研究：
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 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.
体外研究：
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.
PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
体内研究：
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 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.
体外研究：
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.
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