他雷替尼游离碱 T38995

Product Introduction
Bioactivity


英文名: Taletrectinib free base

描述: Taletrectinib free base (AB-106 free base) 是一种新型有效且具有选择性和口服活性的 ROS1/NTRK 抑制剂。Taletrectinib free base 对重组 ROS1、NTRK1、NTRK2 和 NTRK3 具有较强的抑制作用， IC50分别以0.207、0.622、2.28 和 0.98 nM。Taletrectinib free base还对 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变有抑制作用。

体外活性: Taletrectinib free base (1-1000 nM; 72 h) has an IC50 of ~3 -20 nM against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells.[1] Taletrectinib free base (0.001-1000 nM; 2 h) dose-dependently inhibits ROS1 autophosphorylation in U-118-MG cells in vitro.[1] Taletrectinib free base potently inhibits ROS1 autophosphorylation in JFCR-165, JFCR-168 and MGH193-1B cells.[1] Taletrectinib free base partially inhibits phosphorylated NTRK1 at 10 nM and completely inhibits it at 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in an ATP-competitive manner at subnanomolar concentrations. Taletrectinib free base at 0.2 μM almost completely inhibits ACK, ALK, DDR1, and LTK among the 160 kinases but does not strongly inhibit the other 152 kinases in the presence of 1 mM ATP.[1] Taletrectinib free base effectively inhibits crizotinib-resistant ROS1 secondary mutations, including the G2032R solvent front mutation.[1]

体内活性: Taletrectinib free base (DS-6051b) (25 -200 mg/kg; oral; once daily for 18 days; Balb-c nu/nu mice bearing U-118 MG cells) shows anti-tumor activity.[1] Taletrectinib free base (6.25 -200 mg/kg; oral; once daily for 8 days;) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice harboring KM12 cells.[1] Taletrectinib free base (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in wild-type (WT) and G2032R mutant Ba/F3-carrying mice without severe weight loss.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (135.65 mM)


关键字: DS-6051b | IBI 344 | IBI-344 | Taletrectinib | IBI344

相关产品: ROS kinases-IN-2 | APG-2449 | HS-291 | ROS kinases-IN-1 | Anti-inflammatory agent 64 | Crizotinib | Lorlatinib | Uniconazole | F-1 | Taletrectinib

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Bioactive Compound Library

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