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Bafetinib

Chemical Structure : Bafetinib

CAS No.: 859212-16-1

Bafetinib (INNO-406;NS-187)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 576.6154
Formula C30H31F3N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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)-

References

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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