VX-322: A Novel Dual Receptor Tyrosine Kinase Inhibitor for the Treatment of Acute Myelogenous Leukemia

In acute myelogenous leukemia (AML), the FLT3 receptor tyrosine kinase (RTK) is highly expressed with 30% of patients expressing a mutated, constitutively active form of this protein. To inhibit this receptor, VX-322 was developed and found to be very potent against both the FLT3 and c-KIT RTKs with...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-01, Vol.55 (2), p.725-734
Hauptverfasser:	Heidary, David K, Huang, George, Boucher, Diane, Ma, Jianguo, Forster, Cornelia, Grey, Ron, Xu, Jinwang, Arnost, Michael, Choquette, Deborah, Chen, Guanjing, Zhou, Jie-Hua, Yao, Yung-Mae, Ball, Edward D, Namchuk, Mark, Davies, Robert J, Henkel, Greg
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacology Apoptosis - drug effects Cell Survival - drug effects fms-Like Tyrosine Kinase 3 - antagonists & inhibitors Humans Leukemia, Myeloid, Acute - drug therapy Male Mice Mice, Inbred BALB C Morpholines - pharmacology Neoplasm Transplantation Proto-Oncogene Proteins c-kit - antagonists & inhibitors Serum Triazoles - pharmacology Tumor Cells, Cultured
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Zusammenfassung:	In acute myelogenous leukemia (AML), the FLT3 receptor tyrosine kinase (RTK) is highly expressed with 30% of patients expressing a mutated, constitutively active form of this protein. To inhibit this receptor, VX-322 was developed and found to be very potent against both the FLT3 and c-KIT RTKs with enzyme K i values of
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm201198w