化合物Larotrectinib sulfate T6880

Product Introduction
Bioactivity


英文名: Larotrectinib sulfate

描述: 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。

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (94.96 mM)
Ethanol : 10 mg/mL(19 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Larotrectinib sulfate | Inhibitor | LOXO 101 Sulfate | Tropomyosin related kinase receptor | ARRY470 | LOXO101 Sulfate | Trk Receptor | LOXO101 | LOXO 101 | Larotrectinib (LOXO-101) Sulfate | LOXO-101 | Apoptosis | ARRY 470 | LOXO-101 Sulfate | Larotrectinib Sulfate

相关产品: Ispinesib | Furazolidone | Sirtinol | Dabuzalgron | (R)​-​CR8 | Erdafitinib | Wedelolactone | Lysophosphatidylcholines | HDAC-IN-57 | Agrimonolide

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途