产品信息
抗原名称
Bcr-Abl
商品描述
GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).
分子量
418.37
纯度
>98%
可溶性
DMSO ：83 mg/mL (198.38 mM)
Ethanol ：20 mg/mL warmed (47.8 mM)
Ethanol ：20 mg/mL warmed (47.8 mM)
外观
Powder
In vitro(体外研究)
GNF-5, when used in combination with imatinib or nilotinib, suppresses the emergence of resistance mutations in vitro, and displays additive inhibitory activity in biochemical and cellular assays against Bcr-Abl T315I mutant. GNF-5 shows potent antiproliferative activity with EC50 of 430 nM and 580 nM against wt-Bcr-Abl and E255K mutant Bcr-Abl transformed cells, respectively.
In vivo(体内研究)
GNF-5 (100 mg/kg ) displays efficacy on wild-type and T315I Bcr-Abl dependent proliferation in xenograft and bone marrow transplantation models. Moreover, a combination of GNF-5 (75 mg/kg) with nilotinib (50 mg/kg) results in improved overall survival in a T315I Bcr-Abl BMT model.
背景
别名
GNF 5; GNF5
分子式
C20H17F3N4O3
CAS号
778277-15-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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