产品
编 号:F757042
分子式:C39H45N7O3
分子量:659.82
产品类型
结构图
CAS No: 2937544-01-7
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产品详情
生物活性:
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKAG595R, TRKAG667C and TRKAF589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM.
体内研究:
TRK-IN-24 (compound 10g) (50 mg/kg; 10-14 天) 在小鼠的 BaF3-CD74-NTRK1G595R 和 BaF3-CD74-NTRK1G667C 异种移植模型中,处理 10 或 14 天后分别造成 72% 和 78% 的肿瘤消退。
体外研究:
TRK-IN-24 (compound 10g) (3.7-300 nM) 抑制 Ba/F3 细胞中 AKT、TRKA、PLCγ1、ERK 的磷酸化。