化合物 BMS-599626 2HCL(714971-09-2 Free base) T2610L

Product Introduction
Bioactivity


英文名: BMS-599626 2HCL(714971-09-2 Free base)

描述: BMS-599626 2HCL (AC480 2HCl) 是BMS-599626 衍生物。BMS-599626 是一种可口服且具有选择性的 HER1 和 HER2 双重抑制剂， IC50 分别为 20 和 30 nM。BMS-599626 抑制肿瘤细胞增殖，并有可能增加肿瘤对放疗的反应。

体外活性: BMS-599626 is a potent HER inhibitor and has a higher inhibition ability than the other reported inhibitors. When tested with breast tumor cell lines (HCC202, HCC1942 and AU565) that highly expressed HER1 and HER2, BMS-599626 treatment inhibited cell proliferation, while having no effect on A2780 cells without HER1 or HER2 expression.[1] Treated OV202 cells with BMS-599626 significantly inhibited cell proliferation and enhanced cell apoptosis by inhibiting HER.[3] When tested with Sal2 cells expressing CD8-HER2 fusion protein, BMS-599626 treatment inhibited the receptor phosphorylation and MAPK phosphorylation with the IC50 value of 0.3 and 0.22 μM/L, respectively.[1]

体内活性: 在带有Sal2肿瘤细胞异种移植的小鼠模型中，经口给予BMS-599626以剂量依赖的方式抑制了Sal2细胞的生长，并在60 mg/kg的浓度下显著延迟了肿瘤的生长。[1]

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

溶解度: DMSO : 25 mg/mL (41.43 mM)


关键字: BMS-599626 Dihydrochloride | BMS 599626 Dihydrochloride | AC-480 | BMS599626 | BMS599626 Dihydrochloride | BMS 599626 | BMS 599626 dihydrochloride (714971-09-2 free base) | BMS-599626 | AC 480 | AC480

相关产品: Neratinib maleate | Neratinib | Dihydroberberine | HER2/neu (654-662) GP2 acetate | Mollugin | EGFR-IN-99 | PF-04929113 Mesylate | Tucatinib | MCHR1 antagonist 2 | Patritumab

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound 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