Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Larotrectinib 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。
产品描述 | LOXO-101 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 | Larotrectinib (LOXO-101) sulfate, LOXO-101 (sulfate), ARRY-470, Larotrectinib, ARRY-470 (sulfate), LOXO-101 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 2 years
DMSO: 93 mg/mL (176.6 mM)
Ethanol: 10 mg/mL(19 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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。
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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 Larotrectinib (LOXO-101) sulfate Tropomyosin related kinase receptor LOXO-101 (sulfate) LOXO101 ARRY-470 Larotrectinib Trk Receptor ARRY 470 ARRY-470 (sulfate) LOXO-101 LOXO 101 ARRY470 LOXO-101 sulfate inhibitor