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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Bcr-Abl-Bafetinib
Bafetinib

Chemical Structure : Bafetinib

CAS No.: 859212-16-1

Bafetinib (INNO-406;NS-187)

货号: PC-45880Not For Human Use, Lab Use Only.

Bafetinib (INNO-406, NS-187) is a potent and selective dual Abl/Lyn tyrosine kinase inhibitor with IC50 of 5.9 nM and 198 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Bafetinib (INNO-406, NS-187) is a potent and selective dual Abl/Lyn tyrosine kinase inhibitor with IC50 of 5.9 nM and 198 nM, respectively.
Bafetinib is more potent and specific against Bcr-Abl than imatinib, also inhibits the phosphorylation of CrkL and ERK in BaF3/E255K cells.
Bafetinib inhibits the phosphorylation of Bcr-Abl harboring the M244V, G250E, Q252H, Y253F, E255K, E255V, F317L, M351T, E355G, F359V, H396P, or F486S mutations, but does not inhibit the phosphorylation of the T315I mutant.
Bafetinib prolonges the survival of mice injected with leukemic cells expressing all mutated Bcr-Abl.

物理化学性质&存储条件

分子量 576.6154
分子式 C30H31F3N8O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 42 mg/mL

Chemical Name/SMILES

Benzamide, N-[3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl]-4-[[(3S)-3-(dimethylamino)-1-pyrrolidinyl]methyl]-3-(trifluoromethyl)-

参考文献

1. Kimura S, et al. Blood. 2005 Dec 1;106(12):3948-54.

2. Naito H, et al. Leuk Res. 2006 Nov;30(11):1443-6.

3. Yokota A, et al. Blood. 2007 Jan 1;109(1):306-14.

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