Ponatinib (AP24534) hydrochloride 是 ponatinib 的盐酸盐。 Ponatinib 是一种具有口服活性的多靶点激酶抑制剂，对 Abl、PDGFRα、VEGFR2、FGFR1 和 Src 的 IC50 分别为 0.37 nM、1.1 nM、1.5 nM、2.2 nM 和 5.4 nM。
货号:ajcx28388
CAS:1114544-31-8
分子式:C29H27F3N6O • HCl
分子量：569
溶解度:DMF: 2 mg/ml,DMSO: 11 mg/ml,Ethanol: Slightly soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Ponatinib is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor (IC₅₀= 0.37 nM).¹It inhibits the tyrosine kinase inhibitor-resistant mutant Bcr-Abl^T315I(IC₅₀= 2 nM), as well as Bcr-Abl^Q252H, Bcr-Abl^Y253F, Bcr-Abl^M351T, and Bcr-Abl^H396Pmutants (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-Abl^T315Imouse 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)