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PND-1186 hydrochloride

CAS No. : 1356154-94-3

產品活性：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.

研究領域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶點：FAK  |  Apoptosis

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.

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