跳至主要内容

BLU-285 CAS: 1703793-34-3

BLU-285(cas 1703793-34-3)
is a potent and selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants and is being developed as a highly targeted therapy for SM, a disorder of the mast cells in which a KIT Exon 17 mutation is the primary driver of disease. BLU-285 has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (half-maximal inhibitory concentration [IC50] = 0.27 nM). In vivo BLU-285 was well tolerated and has demonstrated dose dependent antitumor efficacy. Complete tumor growth inhibition and ≥ 75% KIT kinase inhibition was observed with 10 mg/kg once daily, oral dosing of BLU-285 in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of disease. BLU-285 is currently in Phase I clinical study.

评论

发表评论

此博客中的热门博文

Custom Synthesis

MuseChem engages in total-support business for research and development of organic compounds for the chemical, pharmaceutical and agrochemical industries. We provide custom manufacturing and process research services on scales ranging from milligrams to kilograms. MuseChem’s scientists in the chemistry team are well trained, can handle even the most complex chemical synthesis and characterization projects, completing the project on your required timeframe. Your inquiry will b e evaluated within a few days to provide you with a quote complemented by a synthetic scheme. The quote is calculated on the basis of the current FTE rate. We deliver detailed biweekly reports with expected delivery dates. Each project is treated under the confidentiality agreement. We won't charge our clients for failed syntheses. We offer high-quality and cost-effective custom synthesis service under strict confidentiality including the following: ● Small-Scale and large scale manufacturing ● Process dev...
发表评论
阅读全文

AP-III-a4 hydrochloride((ENOblock HCl) )|Musechem

AP-III-a4 hydrochloride((ENOblock HCl) )| Musechem ENOblock Hcl(AP-III-a4 Hcl) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.  Enolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell met...
发表评论
阅读全文