NVP-BVU972

一种Met激酶抑制剂(IC50=14nM)；在另外62种激酶中对Met具有选择性（所有激酶的IC50=>1µM）；抑制Met扩增的GTL-16胃癌、MKN45胃癌和EBC-1肺癌细胞的增殖（IC50分别为66、32和82nM）；抑制GTL-16细胞中的Met自身磷酸化和A549细胞中的HGF诱导的Met磷酸化（IC50分别为7.3和22nM）。A Met kinase inhibitor (IC50 = 14 nM); selective for Met over a panel of 62 additional kinases (IC50s = >1 µM for all); inhibits proliferation of Met-amplified GTL-16 gastric, MKN45 gastric, and EBC-1 lung cancer cells (IC50s = 66, 32, and 82 nM, respectively); inhibits Met autophosphorylation in GTL-16 cells and HGF-induced Met phosphorylation in A549 cells (IC50s = 7.3 and 22 nM, respectively).分子式C20H16N6分子量340.4CN(N=C1)C=C1C2=NN3C(C=C2)=NC=C3CC4=CC(C=CC=N5)=C5C=C4