Bafetinib (INNO-406)

Bafetinib (INNO-406)

Catalog Number:
L002369772APE
Mfr. No.:
APE-B1011
Price:
$277
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      • Overview
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          Background

          Bafetinib is a potent and selective dual inhibitor of Bcr-Abl/Lyn tyrosine kinase with IC50 values of 5.8nM and 19nM, respectively [1].
          Bafetinib is a specific dual Abl-Lyn inhibitor. For 79 other tyrosine kinases, 0.1μM bafetinib can inhibit 4 of these enzymes including Abl, Abl-related gene, Fyn and Lyn. Bafetinib can block the autophosphorylation of Bcr-Abl. In K562 and 293T cells transfected with wt Bcr-Abl, bafetinib shows inhibition with IC50 values of 11nM and 22nM, respectively. In the in vitro kinase assays, bafetinib shows inhibition of a variety of Abl kinase mutants such as M244V, G250E, Y253F and F317L. It has no effect on T315I in vitro. Bafetinib also suppresses the growth of Bcr-Abl–positive leukemic cell lines including K562, KU812 and BaF3/wt. The BaF3/E255K cells are also sensitive towards bafetinib. Moreover, bafetinib is highly potent to inhibit tumor growth in murine tumor models [1].

          [1] Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954.

      • Properties
        • Alternative Name
          4-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]methyl]-N-[4-methyl-3-[(5-pyrimidin-5-ylpyrimidin-2-yl)amino]phenyl]-3-(trifluoromethyl)benzamide
          CAS Number
          887650-05-7; 859212-16-1
          Molecular Formula
          C30H31F3N8O
          Molecular Weight
          576.62
          Appearance
          A solid
          Purity
          98.87%
          Solubility
          ≥57.7 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Gabriella R. Sterne. "Signaling mechanisms of Down syndrome cell adhesion molecule in presynaptic arbor size control." University of Michigan.2016.
          2. Sterne, Gabriella R., Jung Hwan Kim, and Bing Ye. "Dysregulated Dscam levels act through Abelson tyrosine kinase to enlarge presynaptic arbors." eLife 4 (2015): e05196. PMID:25988807

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