GZD824

A Bcr/Abl inhibitor

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库存: 现货

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5mg

￥1012.00

810.00

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25mg

￥3112.00

2490.00

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货号: ajci6072
CAS: 1421783-64-3
别名: GZD824 dimesylate; HQP1351 dimesylate
分子式: C29H27F3N6O.2CH4O3S
分子量: 724.77
纯度: >98%
溶解度: ≥ 36.25mg/mL in DMSO
储存: 4°C, away from moisture and light
库存: 现货

Background

GZD824 is an orally bioavailable inhibitor of Bcr-Abl with IC50 values of 0.34 and 0.68 nM for Bcr-AblWT and Bcr-AblT315I, respectively [1].

Bcr-Abl is a fused protein that interacts with the interleukin-3 receptorβ(c) subunit and has tyrosine kinase activity. Abl activates cell cycle-related proteins and enzymes and increases cell division. Bcr-Abl inhibits DNA repair and causes genomic instability.

GZD824 is an orally bioavailable Bcr-Abl inhibitor. GZD824 exhibited high affinity with Kd values of 0.32 and 0.71 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GZD824 inhibited Bcr-Abl with IC50 values of 0.34, 0.68, 0.27, 0.71, 0.15, 0.35, 0.29 and 0.35 nM for Bcr-AblWT, Bcr-AblT315I, Bcr-AblE255K, Bcr-AblG250E, Bcr-AblQ252H, Bcr-AblH396P, Bcr-AblM351T and Bcr-AblY253F, respectively. In a competitive binding assay, GZD824 bound to the ATP-binding sites of native Abl with Kd values of 0.32 and 0.34 nM for non-phosphorylated and phosphorylated Abl. In stably transformed Ba/F3 cells, GZD824 potently inhibited cells growth with IC50 values of 1.0 and 7.1 nM for Bcr-AblWT and Bcr-AblT315I expressed cells, respectively [1].

In mouse xenograft tumor models, GZD824 inhibited tumor growth. In mice bearing an allograft leukemia model, GZD824 significantly increased survival [1].

Reference:
Ren X, Pan X, Zhang Z, et al.? 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, 56(3): 879-894.