Flumatinib mesylate

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Chemical Structure| 895519-91-2 同义名 : 氟马替尼 ;HHGV678 mesylate
CAS号 : 895519-91-2
货号 : A494480
分子式 : C30H33F3N8O4S
纯度 : 99%+
分子量 : 658.694
MDL号 : MFCD28053502
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(75.91 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(75.91 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Flumatinib mesylate (HH-GV-678) is an oral, selective inhibitor of Bcr-Abl, inhibiting c-Abl, PDGFRβ, and c-Kit with IC50 values of 1.2, 307.6, and 665.5 nM, respectively. It inhibits Bcr-Abl autophosphorylation and phosphorylation of Stat5 and Erk1/2, impeding tumor growth in a chronic myelogenous leukemia model [1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.52mL

0.30mL

0.15mL

7.59mL

1.52mL

0.76mL

15.18mL

3.04mL

1.52mL

参考文献

[1]Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9.

[2]Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10.