化合物ASP 3026 T1962

Product Introduction
Bioactivity


英文名: ASP3026

描述: ASP3026 是一种选择性的，具有口服活性的间变性淋巴瘤激酶抑制剂，可诱导肿瘤细胞凋亡，可研究非小细胞肺癌。

激酶实验: Recombinant truncated FLAG-tagged mTOR expressed in HEK 293 cells is used in biochemical assays, together with a biotinylated p70S6K peptide substrate. Streptavidin donor and protein A acceptor beads are used to assemble the capture complex for generation of the assay signal. The activity of the lipid kinases, PI3K alpha, beta, delta, and gamma are measured using recombinant proteins and the lipid PIP2 as substrate. Assays for ATM and DNA-PK activity are performed. The mTOR cellular activity is measured in MDAMB468 cells, using an Acumen laser scanning cytometer to analyze the levels of phosphorylation of S6 (Ser235/236) and AKT (Ser473)[1].

体外活性: 以每天两次口服给药ASP3026的方式处理荷有皮下NCI-H2228肿瘤异种移植物的小鼠14天,诱导剂量依赖性的抗肿瘤作用,从1 mg/kg开始,在10,30和100 mg/kg强烈消退.

体内活性: ASP3026抑制内源性表达EML4-ALK变体3的人NSCLC肿瘤细胞系NCI-H2228的生长,IC50值为64.8 nM。ASP3026在酪氨酸激酶中比PF02341066显示更强的选择性抑制ALK活性。

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

溶解度: DMSO : 11.6 mg/mL (20 mM)


关键字: inhibit | ALK tyrosine kinase receptor | Anaplastic lymphoma kinase (ALK) | Apoptosis | Inhibitor | ASP-3026 | Cluster of differentiation 246 | ASP3026 | Anaplastic lymphoma kinase | CD246

相关产品: RUNX-IN-2 | TMI-1 | T0901317 | Entinostat | Deoxypodophyllotoxin | Metronidazole | PYR-41 | Antitumor agent-103 | Chetomin | Indirubin

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Bioactive Compound 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