Bafetinib (1-10 μM) concentration dependently inhibits PAR2-TRPV4 coupling. In TRPV4 HEKs, 10 μM Bafetinib significantly inhibits the coupling response to SLIGRL and trypsin compared with vehicle control. Bafetinib inhibits the signalling pathway leading
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Tyrosine-protein kinase Lyn inhibitor
Note
Refer to SDS for further information Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.
1.Horio T, Hamasaki T, Inoue T, Wakayama T, Itou S, Naito H, Asaki T, Hayase H, Niwa T. (2007) Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.. Bioorg Med Chem Lett, 17 (10):(2712-7). [PMID:17376680]
2.Rix U, Remsing Rix LL, Terker AS, Fernbach NV, Hantschel O, Planyavsky M, Breitwieser FP, Herrmann H, Colinge J, Bennett KL et al.. (2010) A comprehensive target selectivity survey of the BCR-ABL kinase inhibitor INNO-406 by kinase profiling and chemical proteomics in chronic myeloid leukemia cells.. Leukemia, 24 (1):(44-50). [PMID:19890374]
4.Kantarjian H, le Coutre P, Cortes J, Pinilla-Ibarz J, Nagler A, Hochhaus A, Kimura S, Ottmann O. (2010) Phase 1 study of INNO-406, a dual Abl/Lyn kinase inhibitor, in Philadelphia chromosome-positive leukemias after imatinib resistance or intolerance.. Cancer, 116 (11):(2665-72). [PMID:20310049]
5.Santos FP, Kantarjian H, Cortes J, Quintas-Cardama A. (2010) Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia.. Curr Opin Investig Drugs, 11 (12):(1450-65). [PMID:21154127]
6.Kimura S, Naito H, Segawa H, Kuroda J, Yuasa T, Sato K, Yokota A, Kamitsuji Y, Kawata E, Ashihara E et al.. (2005) NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia.. Blood, 106 (12):(3948-54). [PMID:16105974]
7.Sterne GR et al.. (2015) Dysregulated Dscam levels act through Abelson tyrosine kinase to enlarge presynaptic arbors.. Elife, 4 [PMID:25988807]
8.Yokota A et al.. (2007) INNO-406, a novel BCR-ABL/Lyn dual tyrosine kinase inhibitor, suppresses the growth of Ph+ leukemia cells in the central nervous system, and cyclosporine A augments its in vivo activity.. Blood, 109 (306-14). [PMID:16954504]
9.Kamitsuji Y et al.. (2008) The Bcr-Abl kinase inhibitor INNO-406 induces autophagy and different modes of cell death execution in Bcr-Abl-positive leukemias.. Cell Death Differ, 15 (11):(1712-22). [PMID:18617896]
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K2216083