NVP-BVU972

  Cat. No.:  DC8743  
Chemical Structure
1185763-69-2
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More than 5000 active chemicals with high quality for research!
Field of application
NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.
Cas No.: 1185763-69-2
Synonyms: NVP-BVU 972
SMILES: CN1N=CC(C2C=CC3N(C(CC4C=CC5N=CC=CC=5C=4)=CN=3)N=2)=C1
Formula: C20H16N6
M.Wt: 340.38
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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