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Olverembatinib
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Olverembatinib图片
CAS NO:1257628-77-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
GZD824 (HQP1351) 是一种高效的，具有口服活性的 pan-Bcr-Abl 抑制剂。GZD824 能广泛而有效地抑制突变型 Bcr-Abl。GZD824 对天然的 Bcr-Abl 和 Bcr-AblT315I 作用的 IC50 值分别为 0.34 nM 和 0.68 nM。GZD824 具有抗肿瘤作用。
Cas No.1257628-77-5
别名GZD824; HQP1351
分子式C29H27F3N6O
分子量532.56
溶解度DMSO : ≥ 100 mg/mL (187.77 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GZD824 (HQP1351) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity[1].

GZD824 shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].GZD824 selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].GZD824 inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-AblT315I(0.1-100 nM; 4.0 hours)[1].

GZD824 suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT[1].GZD824 (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-AblT315I[1].GZD824 exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].GZD824 exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg)[1].

[1]. Ren X, Pan X, Zhang Z, Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem. 2013 Feb 14;56(3):879-94.