2412055-93-5
中文名稱
化合物CG 428
英文名稱
1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-
CAS
2412055-93-5
分子式
C43H43FN10O6
分子量
814.86
MOL 文件
2412055-93-5.mol
2412055-93-5 結(jié)構(gòu)式
基本信息
中文別名
化合物CG 428化合物CG 428,10 MM DMSO 溶液
英文別名
CG 4281H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-
物理化學性質(zhì)
密度1.51±0.1 g/cm3(Predicted)
溶解度Soluble to 100 mM in DMSO
酸度系數(shù)(pKa)10.74±0.40(Predicted)
應(yīng)用領(lǐng)域
用途一
CG428 is a tropomyosin receptor kinase (TRK) degrader that targets the intracellular kinase domain of TRK. CG428 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells and inhibited downstream PLCγ1 signaling at sub-nanomolar concentrations. CG428 also degraded human wild-type TRKA.