Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Selitrectinib (LOXO-195) 是二代原肌凝蛋白相关激酶(TRK)抑制剂,能够作用于 TRKA (IC50:0.6 nM) 和 TRKC (IC50<2.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 347 | 现货 | ||
5 mg | ¥ 798 | 现货 | ||
10 mg | ¥ 1,220 | 现货 | ||
25 mg | ¥ 2,380 | 现货 | ||
50 mg | ¥ 3,560 | 现货 | ||
100 mg | ¥ 4,760 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 892 | 现货 |
产品描述 | Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively) |
靶点活性 | TrkA:0.6 nM , TrkC:<2.5 nM |
体内活性 | Selitrectinib (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models. |
动物实验 | Each cell line (2–5×10e6 cells) was injected subcutaneously into female nu/nu NCr mice age 7–9 weeks and allowed to grow to ~100–200 mm3 (efficacy) or ~ 500mm3 (PK-PD) prior to randomization by tumor size and treatment with each inhibitor by oral gavage.?For PK-PD analysis, animals were dosed for 3 days, followed by euthanasia, excision of tumors and collection of plasma.?Phospho-TRK levels in tumor lysates were determined by ELISA assay, while plasma inhibitor levels were determined by LC-MS/MS.?For efficacy analysis, animals were dosed by oral gavage, and body weight and tumor size were monitored at regular intervals. |
别名 | LOXO-195 |
分子量 | 380.42 |
分子式 | C20H21FN6O |
CAS No. | 2097002-61-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 62.5 mg/mL (164.29 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6287 mL | 13.1434 mL | 26.2867 mL | 65.7168 mL |
5 mM | 0.5257 mL | 2.6287 mL | 5.2573 mL | 13.1434 mL | |
10 mM | 0.2629 mL | 1.3143 mL | 2.6287 mL | 6.5717 mL | |
20 mM | 0.1314 mL | 0.6572 mL | 1.3143 mL | 3.2858 mL | |
50 mM | 0.0526 mL | 0.2629 mL | 0.5257 mL | 1.3143 mL | |
100 mM | 0.0263 mL | 0.1314 mL | 0.2629 mL | 0.6572 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。
Selitrectinib 2097002-61-2 Tyrosine Kinase/Adaptors Trk receptor LOXO195 Inhibitor LOXO 195 Tropomyosin related kinase receptor LOXO-195 Trk Receptor inhibit inhibitor