Ponatinib HCl

Ponatinib is an orally bioavailable multitargeted receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor AP24534 inhibits unmutated and all mutated forms of Bcr-Abl, including T315I, the highly drug therapy-resistant missense mutation of Bcr-Abl. This agent also inhibits other tyrosine kinases including those associated with vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs); in addition, it inhibits the tyrosine kinase receptor TIE2 and FMS-related tyrosine kinase receptor-3 (Flt3).

Product information

CAS Number: 1114544-31-8

Molecular Weight: 569.02

Formula: C29H28ClF3N6O

Synonym:

AP24534

Ponatinib HCl

Ponatinib hydrochloride. trade name Iclusig

Chemical Name: 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide hydrochloride

Smiles: Cl.CN1CCN(CC2=CC=C(C=C2C(F)(F)F)NC(=O)C2=CC=C(C)C(=C2)C#CC2=CN=C3C=CC=NN23)CC1

InChiKey: BWTNNZPNKQIADY-UHFFFAOYSA-N

InChi: InChI=1S/C29H27F3N6O.ClH/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37;/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39);1H

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Oaxaca DM, Yang-Reid SA, Ross JA, Rodriguez G, Staniswalis JG, Kirken RA. Sensitivity of imatinib-resistant T315I BCR-ABL CML to a synergistic combination of ponatinib and forskolin treatment. Tumour Biol. 2016 Jul 21. [Epub ahead of print] PubMed PMID: 27444277.
2. Abid MB, De Mel S. Does ponatinib cross the blood-brain barrier? Br J Haematol. 2016 Jun 28. doi: 10.1111/bjh.14222. [Epub ahead of print] PubMed PMID: 27352067.
3. Engel NW, Constantin A, Fowlkes S, Assouline S. Unexpected Success of Watch and Wait Strategy in a Ponatinib-Intolerant Patient With Chronic Myeloid Leukemia. J Oncol Pract. 2016 Jun;12(6):592-4. doi: 10.1200/JOP.2016.012054. Epub 2016 May 31. PubMed PMID: 27246687.

Products are for research use only. Not for human use.