Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 455 | 现货 | ||
5 mg | ¥ 1,110 | 现货 | ||
10 mg | ¥ 1,780 | 现货 | ||
25 mg | ¥ 3,590 | 现货 | ||
50 mg | ¥ 5,180 | 现货 | ||
100 mg | ¥ 7,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,350 | 现货 |
产品描述 | Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1/NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations. |
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] |
别名 | AB-106freebase, Taletrectinib free base, IBI-344 free base, DS-6051b free base |
分子量 | 405.47 |
分子式 | C23H24FN5O |
CAS No. | 1505514-27-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (135.65 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4663 mL | 12.3314 mL | 24.6627 mL | 61.6568 mL |
5 mM | 0.4933 mL | 2.4663 mL | 4.9325 mL | 12.3314 mL | |
10 mM | 0.2466 mL | 1.2331 mL | 2.4663 mL | 6.1657 mL | |
20 mM | 0.1233 mL | 0.6166 mL | 1.2331 mL | 3.0828 mL | |
50 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2331 mL | |
100 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Taletrectinib free base 1505514-27-1 Tyrosine Kinase/Adaptors ROS Kinase AB-106freebase DS-6051b IBI 344 IBI-344 Taletrectinib IBI-344 free base DS-6051b free base IBI344 Inhibitor inhibitor inhibit