Ponatinib (hydrochloride) (Synonyms: AP 24534) |
رقم الكتالوجGC52104 |
Ponatinib (AP24534) هيدروكلوريد هو هيدروكلوريد البوناتينيب. Ponatinib هو مثبط كيناز متعدد الأهداف فعال عن طريق الفم مع IC50s من 0.37 نانومتر و 1.1 نانومتر و 1.5 نانومتر و 2.2 نانومتر و 5.4 نانومتر لـ Abl و PDGFRα و VEGFR2 و FGFR1 و Src ، على التوالي.
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Cas No.: 1114544-31-8
Sample solution is provided at 25 µL, 10mM.
Ponatinib is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor (IC50 = 0.37 nM).1 It inhibits the tyrosine kinase inhibitor-resistant mutant Bcr-AblT315I (IC50 = 2 nM), as well as Bcr-AblQ252H, Bcr-AblY253F, Bcr-AblM351T, and Bcr-AblH396P mutants (IC50s = 0.44, 0.3, 0.3, and 0.34 nM, respectively). It is selective for Bcr-Abl and these mutants over the insulin receptor, IGF-1R, Aurora A kinase, and Cdk2/cyclin E but does inhibit the receptor tyrosine kinases c-Src, VEGF receptor 2 (VEGFR2), FGFR1, and PDGFRα (IC50s = 5.4, 1.5, 2.2, and 1.1 nM, respectively). Ponatinib inhibits proliferation of Ba/F3 cells expressing native (IC50 = 0.5 nM) or mutant Bcr-Abl (IC50s = 0.5-36 nM) and induces apoptosis. It reduces tumor growth in a Ba/F3 Bcr-AblT315I mouse xenograft model when administered at doses ranging from 10 to 30 mg/kg. Formulations containing ponatinib have been used in the treatment of chronic-, accelerated-, or blast-phase chronic myeloid leukemia (CML), T315I-positive CML, or T315I-positive Philadelphia-chromosome positive acute lymphoblastic leukemia (Ph+ ALL).
1.O’Hare, T., Shakespeare, W.C., Zhu, X., et al.AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistanceCancer Cell16(5)401-412(2009)
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