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BIOLOGICAL INFO
Solubility:
DMSO =105mg/mL, Water <1.2mg/mL, Ethanol =105mg/mL
Application(s):
Multi-target inhibitor of Abl, PDGFRa, VEGFR2, FGFR1 and Src
Form:
Free base
Research Area:
Leukemia
REVIEW Ponatinib (AP24534) is a novel potent, orally available small molecule multitargeted kinase inhibitor and its primary cellular target is the Bcr-Abl tyrosine kinase protein which is constitutively active and promotes the progression of CML. Ponatinib is unique in that it is especially useful in the treatment of resistant CML because it inhibits the tyrosine kinase activity of Abl and T315I mutant kinases. Other targets that ponatinib inhibits are members of the VEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2, and FLT3.
REFERENCES
[1]
Pound, H. B.; Ho, V. Q.; Pinilla-Ibarz, J. Ponatinib: multitargeted kinase inhibitor pan-BCR-ABL inhibitor oncolytic: AP-24534. Drugs of the Future. (2011) 36(11): 807-812.
[2]
Narayanan V, Pollyea DA, Gutman JA, Jimeno A. Ponatinib for the treatment of chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia. Drugs Today (Barc). (2013) Apr;49(4): 261-9.
[3]
Thomas, Xavier. Is AP24534 (Ponatinib) the next treatment for Philadelphia chromosome-positive acute lymphoblastic leukemia? Bulletin du Cancer. (2011) 98(7): 761-767.
[4]
Zou, Dong; Huang, Wei-Sheng; Thomas, R. Mathew; Romero, Jan Antionette C.; Qi, Jiwei; Wang, Yihan; Zhu, Xiaotian; Shakespeare, William C.; Sundaramoorthi, Rajeswari; Metcalf, Chester A., III; et al Preparation of bicyclic heteroaryl alkynyl arenes as protein kinase inhibitors for treatment of cancer PCT Int. Appl. (2007), WO 2007075869 A2 20070705.
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