NVP-BVU972是一种有效的，选择性的Met抑制剂，IC50为14 nM。NVP-BVU972有效抑制MET激酶，而对其他激酶包括最密切相关的激酶RON抑制作用很低，IC50为1000 nM以上。NVP-BVU972作用于GTL-16细胞，抑制组成型MET磷酸化，作用于A549细胞，抑制HGF刺激的MET磷酸化，IC50分别为7.3和 22 nM。NVP-BVU972 有效抑制MET 基因扩散的细胞系GTL-16, MKN-45和EBC-1生长，IC50分别为66, 82 和 32 nM。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

NVP-BVU 972

Ethanol ：63 mg/mL (185.1 mM)

DMSO ：63 mg/mL (185.1 mM)

Met

NVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more than 1000 nM. NVP-BVU972 also suppresses constitutive MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 nM and 22 nM, respectively. NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC50 values of 66 nM, 82 nM and 32 nM, respectively. In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations give rise to dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell line. Resistance triggered by V1155L is more limited to NVP-BVU972. A dose-dependent reduction in TPR-MET phosphorylation when applying NVP-BVU972 to BaF3 cells expressing wild-type TPR-MET. Both Y1230H and D1228A mutations abrogated the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interferes with the potency of NVP-BVU972 to prevent TPR-MET phosphorylation.