Cas No.: | 1001917-37-8 |
Chemical Name: | 5H-Benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide, 3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)- |
Synonyms: | MK 8033;MK8033 |
SMILES: | CN1C=C(C2=CN=C3C=CC4C=CC(CS(NCC5C=CC=CN=5)(=O)=O)=CC=4C(=O)C3=C2)C=N1 |
Formula: | C25H21N5O3S |
M.Wt: | 471.530943632126 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM; MK-8033 is >100-fold selective relative to Ron and c-Met inhibition against a panel of 221 kinases; potently and selectively inhibits growth in c-Met amplified cell lines (GTL-16 proliferation IC50 =582 nM), causes full inhibition of tumor growth in c-Met amplified (GTL-16) subcutaneous tumor xenograft model; synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Solid Tumors Phase 1 Clinical |