诺华的cMET新药INC280

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本帖最后由老马于 2013-4-29 02:59 编辑

Name:  INC280，INCB28060
CAS#:  1029712-80-8, 1029714-89-3 (XHCl), 1197376-85-4 (2HCl)
Chemical Formula: C23H17FN6O
Exact Mass: 412.14479
Molecular Weight: 412.42
Elemental Analysis: C, 66.98; H, 4.15; F, 4.61; N, 20.38; O, 3.88
IUPAC/Chemical name:
2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide

A Safety and Efficacy Study of INC280 and Gefitinib in Patients With EGFR Mutated, c-MET-amplified NSCLC Who Have Progressed After EGFRi Treatment
中国广州有临床试验
http://clinicaltrials.gov/show/NCT01610336
INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases.
专利WO2009/106577 EN 2009.09.03中第80个实施例，cMET IC50=38nM。
Xl184 cMET IC50=1.3nM
Xalkori cMET IC50=8nM

INC280动物试验数据.PDF (1.76 MB, 下载次数: 819)

INC280中文专利（诺华）.part2.rar (787.78 KB, 下载次数: 1303)

INC280中文专利（诺华）.part1.rar (1.39 MB, 下载次数: 1393)