1163719-91-2
中文名稱
化合物CCT241161
英文名稱
CCT241161
CAS
1163719-91-2
分子式
C28H27N7O3S
分子量
541.62
MOL 文件
1163719-91-2.mol
1163719-91-2 結(jié)構(gòu)式
基本信息
中文別名
化合物CCT241161 英文別名
CCT2411611-(5-tert-butyl-2-phenylpyrazol-3-yl)-3-[2-methylsulfanyl-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea
N-[4-[(3,4-dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-(methylthio)phenyl]-N'-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]-urea
Urea, N-[4-[(3,4-dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-(methylthio)phenyl]-N'-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]-
物理化學(xué)性質(zhì)
密度1.36±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度可溶于DMSO
酸度系數(shù)(pKa)8.47±0.20(Predicted)
形態(tài)固體
應(yīng)用領(lǐng)域
用途一
CCT241161 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. CCT241161 blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK?–ERK, in vitro and in vivo. CCT241161 also prevented growth of xenografts derived from patient tumours with acquired or intrinsic resistance to BRAF and MEK inhibitors. BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs.常見問題列表
概述
CCT241161 是一種口服有效的泛型 RAF 抑制劑，其對(duì) LCK, CRAF, SRC, V600E-BRAF 和 BRAF 的 IC50 值分別為 3, 6, 10, 15 和 30 nM。CCT241161 對(duì) BRAF 和 NRAS 突變的黑色素瘤具有良好的活性。CCT241161 還具有抗癌細(xì)胞增殖活性。