N-甲基-N-[2-[[[2-[(2-氧代-2,3-二氫-1H-吲哚-5-基)氨基
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產(chǎn)品名稱:N-甲基-N-[2-[[[2-[(2-氧代-2,3-二氫-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]苯基]甲磺酰胺CAS:717906-29-1別名:N-甲基-N-[2-[[[2-[(2-氧代-2,3-二氫-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]苯基]甲磺酰胺;PF-431396;PF431396英文名:N-Methyl-N-[2-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide - 生物活性PF-431396是雙PYK2/FAK抑制劑,IC50分別為11nM和2 nM。
- 體外研究In A20 cells, PF-431396 blocks anti-Ig- and clustering LFA-1-induced tyrosine phosphorylation of Pyk2 and FAK, and further blocks B cell spreading. PF-431396 consistently inhibits the increase in protein tyrosine phosphorylation (PY) induced by the absence of added calcium and induced by W-7 in the presence of calcium.