Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Larotrectinib sulfate (LOXO-101 sulfate) 是一种 ATP 竞争性的,口服选择性抑制剂,对原肌凝蛋白相关激酶家族受体的三个亚型具有纳摩尔级别的 50% 抑制浓度。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 655 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,280 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
500 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 759 | 现货 |
产品描述 | Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
体外活性 | LOXO-101(ARRY-470) is a specific kinase inhibitor with nanomolar activity against TRKA/TRKB/TRKC but no other notable kinase inhibition (1 μM). ARRY-470 hasn't the inhibitory of the proliferation of Ba/F3 cells expressing other oncogene targets (EGFR, ROS1 or ALK) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells. |
体内活性 | Early/sustained but not late/acute administration of ARRY-470(LOXO-101) obviously attenuates bone cancer pain and blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor-bearing bone, but no significant inhibition for tumor growth or bone remodeling. It has very limited ability crossing of the blood-brain barrier. |
细胞实验 | Concentrations: 10,100,1000 nM. Method: Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G,gefitinib 1,000 nM) or DMSO control.The cell lysate is used for western blot analysis. |
动物实验 | Animal Models: Adult male C3H/HeJ mice. Formulation: Labrafac; polygly-colyzed glyceride. Dosages: 10-100 mg/kg. Administration: p.o. |
别名 | LOXO-101 sulfate, Larotrectinib (LOXO-101) sulfate, Larotrectinib, LOXO-101 (sulfate), ARRY-470, ARRY-470 (sulfate) |
分子量 | 526.51 |
分子式 | C21H22F2N6O2·H2O4S |
CAS No. | 1223405-08-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (176.6 mM)
Ethanol: 10 mg/mL(19 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.8993 mL | 9.4965 mL | 18.993 mL | 47.4825 mL |
5 mM | 0.3799 mL | 1.8993 mL | 3.7986 mL | 9.4965 mL | |
10 mM | 0.1899 mL | 0.9496 mL | 1.8993 mL | 4.7482 mL | |
DMSO | 20 mM | 0.095 mL | 0.4748 mL | 0.9496 mL | 2.3741 mL |
50 mM | 0.038 mL | 0.1899 mL | 0.3799 mL | 0.9496 mL | |
100 mM | 0.019 mL | 0.095 mL | 0.1899 mL | 0.4748 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。
Larotrectinib sulfate 1223405-08-0 Apoptosis Tyrosine Kinase/Adaptors Trk receptor inhibit Inhibitor LOXO 101 Sulfate Tropomyosin related kinase receptor LOXO-101 sulfate ARRY470 LOXO101 Sulfate Larotrectinib (LOXO-101) sulfate Trk Receptor Larotrectinib LOXO-101 (sulfate) LOXO101 LOXO 101 Larotrectinib (LOXO-101) Sulfate LOXO-101 ARRY-470 ARRY 470 ARRY-470 (sulfate) LOXO-101 Sulfate Larotrectinib Sulfate inhibitor