Olverembatinib dimesylate

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Chemical Structure| 1421783-64-3 同义名 : GZD824 dimesylate; HQP1351 dimesylate
CAS号 : 1421783-64-3
货号 : A423528
分子式 : C31H35F3N6O7S2
纯度 : 98%
分子量 : 724.77
MDL号 : MFCD26142656
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(165.57 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(68.99 mM)
生物活性
靶点

  • Abl

    Abl, IC50:0.34 nM

    Abl (G250E), IC50:0.35 nM
描述 GZD824 dimesylate is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.38mL

0.28mL

0.14mL

6.90mL

1.38mL

0.69mL

13.80mL

2.76mL

1.38mL
参考文献

[1]Ren X, Pan X, 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 Feb 14;56(3):879-94.