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Ponatinib is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor (IC50 = 0.37 nM).{25003} 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 PDGFR? (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).
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 g, 100 mg, 50 mg, 500 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1114544-31-8 |
| Molecular formula | C29H27F3N6O • HCl |
| Smiles | O=C(C1=CC=C(C)C(C#CC2=CN=C3C=CC=NN23)=C1)N([H])C4=CC=C(CN5CCN(CC5)C)C(C(F)(F)F)=C4.Cl |
| Molecular weight | 569 |
| Custom code | 2933.59 |
| Formulation | A solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
This mixture contains the primary metabolites of prostaglandins (PGs) D2, E2, and F2?. Contents: 13,14-dihydro-15-keto PGD2, 13,14-dihydro-15-keto PGE2, 11?-PGF2?, 13,14-dihydro-15-keto...
Cytosolic PGE synthase (cPGES) is a glutathione-dependent enzyme with a predicted size of 18.6 kDa (23 kDa on SDS-PAGE). The...
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This mixture contains primary prostaglandins produced from arachidonic acid and dihomo-?-linolenic acid. Contents: Prostaglandin E1, Prostaglandin E2, Prostaglandin F1?, 6-keto...
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The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
Endocannabinoids, such as arachidonoyl ethanolamide (AEA) and 2-arachidonoyl glycerol (2-AG), function as short-range modulators of cell and synaptic activity. Monoacylglycerol...
Secretory phospholipase A2 (sPLA2) (Type IIA) is a calcium-dependent PLA2 superfamily member that is encoded by PLA2G2A in humans.{56210} It...
Nuclear factor erythroid 2-related factor 2 (Nrf2) is a basic leucine zipper transcription factor encoded by NFE2L2 in humans that...
The cyclopentenone prostaglandin HPLC mixture contains all of the major UV-absorbing cyclopentenone prostaglandins and their precursors supplied in methyl acetate....
CD34 is a transmembrane phosphoglycoprotein and sialomucin protein that is commonly used as a marker for hematopoietic progenitor cells.{59706,59704} It...
This rabbit anti-mouse IgA FITC is used as the ‘secondary antibody’ for immunostaining experiments where the primary antibody is mouse...
Adenosine Receptor A2A is a multi-pass membrane protein that is normally localized to the plasma membrane.{15465} This receptor is part...
Protein phosphorylation is an important post-translational modification that serves many key functions to regulate a protein’s activity, localization, and protein-protein...
(+)-D-threo-PDMP is a ceramide analog and is one of the four possible stereoisomers of PDMP (Item No. 62595).{11392} (+)-D-threo-PDMP is...
This mixture contains the primary COX products produced by most mammalian tissues. Contents: Prostaglandin D2, Prostaglandin E2, 6-keto Prostaglandin F1?,...
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