PND-1186 hydrochloride (Synonyms: VS-4718 hydrochloride; SR-2516 hydrochloride) |
| カタログ番号GC62111 |
PND-1186 塩酸塩 (VS-4718 塩酸塩) は、IC50 が 1.5 nM の、強力で特異性の高い、可逆的な FAK 阻害剤です。 PND-1186 塩酸塩は、腫瘍細胞のアポトーシスを選択的に促進します。
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Cas No.: 1356154-94-3
Sample solution is provided at 25 µL, 10mM.
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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[1].
PND-1186 has an IC50 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].
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].
[1]. Tanjoni I, et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.
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