Name | AP 24534 |
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Supplier | Tocris Bioscience |
Catalog | 3296 |
Prices | $245.00, $1,005.00 |
Sizes | 10 mg, 50 mg |
Function Type | Inhibitor |
Cas Number | 943319-70-8 |
Chemical Name | 3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-benzamide |
Formula | C29H27F3N6O |
Molecular Weight | 532.56 |
Purity | >98 % |
Description | Potent multi-kinase and pan-Bcr-Abl inhibitor. Displays potent activity against cell lines expressing native Bcr-Abl or Bcr-Abl T3151 (IC 50 values are 0.37 and 2.0 nM respectively); also inhibits other Abl kinase domain mutants at nanomolar potencies. Exhibits inhibitory activity against PDGFR α , c-Src and c-Kit (IC 50 values are 1.1, 5.4 and 12.5 nM respectively); potently inhibits FGFR and VEGFR family kinases. Orally active. |
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O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T. Cancer Cell. 2009 Nov 6;16(5):401-12.
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC. J Med Chem. 2010 Jun 24;53(12):4701-19.
Gozgit JM, Wong MJ, Wardwell S, Tyner JW, Loriaux MM, Mohemmad QK, Narasimhan NI, Shakespeare WC, Wang F, Druker BJ, Clackson T, Rivera VM. Mol Cancer Ther. 2011 Jun;10(6):1028-35.