Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1]. |
体外活性 | NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers [1]. Trk-IN-20 (compound 7mb) (0.031, or 0.018 μM, respectively; 72 h) exhibits strong inhibition against the Larotrectinib-resistant cells with NTRK1-G667C or NTRK3-G696A mutations with IC 50 s of 0.031 and 0.018 μM, respectively [1]. Trk-IN-20 (compound 7mb) (9-22 nM; 72 h) inhibits BaF3 murine cells stably transformed with NTRK oncogenic fusions including CD74-NTRK1, ETV6-NTRK2 and ETV6-NTRK3 with IC 50 s of 15, 22, and 9 nM, respectively [1]. Trk-IN-20 (compound 7mb) (0.32, 1.6, 8, 40, 200; 6 h) inhibits activation of Trk and its downstream proteins in BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells [1]. Trk-IN-20 (compound 7mb) tightly bound to ATP-binding site of TrkA, TrkB, and TrkC with binding constant (K d ) values of 1.6, 3.1 and 4.9 nM, respectively [1]. Western Blot Analysis [1] Cell Line: BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells Concentration: 0, 0.32, 1.6, 8, 40, 200 nM Incubation Time: 6 hours Result: Inhibited the phosphorylation of TrkA/B/C and their downstream signaling molecules ERK, AKT, and PLC-γ1. And also induced partial degradation of Trk protein in BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells. |
体内活性 | Trk-IN-20 (compound 7mb) (p.o.; 10 mg/kg) shows short half-life of 1.39 hours and a low oral bioavailability of 8.79% in rats [1]. Animal Model: Pharmacokinetic Profile of Trk-IN-20 (Compound 7mb) in Rats [1] Dosage: Administration: Result: Route Dose (mg/kg) AUC 0-∞ (μM.h) C max (μM) T 1/2 (h) CL (L/h/kg) BA (%) i.v. 2 3.69 6.77 1.39 1.44 / p.o. 10 1.62 0.36 1.13 - 8.79 |
分子量 | 376.4 |
分子式 | C22H18F2N4 |
CAS No. | 2460924-63-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Trk-IN-20 2460924-63-2 Inhibitor inhibitor inhibit