Chemical Property of Ponatinib
Chemical Property:
- PKA:12.99±0.70(Predicted)
- PSA：65.77000
- Density:1.292 g/cm3
- LogP:4.40480
- Storage Temp.:-20°C
- Solubility.:Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml with warming).
- Purity/Quality:
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99%, *data from raw suppliers
AP 24534 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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Drug Interactions
CYP3A4 enzyme can promote the metabolism of ponatinib. So during the treatment, we should avoid using potent CYP3A4 inhibitors. Information related to the pharmacological effects, side effects, drug contraindications, etc of ponatinib is edited by Shiyan from lookchem. (2015-10-23)
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Description
Ponatinib (943319-70-8) is a highly potent pan-Bcr-Abl and multikinase inhibitor, suppressing the activity of native Bcr-Abl (IC50=0.37 nM) as well as the mutants T315I (IC50=2 nM), Q252H (IC50=0.44 nM), Y253F (IC50=0.3 nM), M351T (IC50=0.3 nM) and H396P (IC50=0.34 nM).1??Also inhibits PDGFRα, c-Src and c-Kit (IC50=1.1, 5.4 and 12.5 nM respectively)2?as well as FGFR-mediated signaling (IC50<40 nM)3. Protects against influenza A virus-induced death by suppressing cytokine storm in mouse models..4
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Uses
AP24534 is a novel potent, orally available small molecule multitargeted kinase inhibitor with IC50 of 0.37, 2, 1.5, 2.2, 1.1, 1and 0.24 nM for native pan-BCR-ABL, mutated form, VEGFR2, FGFR1, PDGFRα, mutant FLT3 phosphorylation and LYN. Ponatinib (AP24534) is a novel potent, orally available small molecule multitargeted kinase inhibitor. Ponatinib inhibits both native and mutant BCR-ABL. Ponatinib is used in the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors. Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively
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Clinical Use
Protein kinase inhibitor:
Treatment of chronic myeloid leukaemia (CML)
Treatment of Philadelphia chromosome positive
acute lymphoblastic leukaemia (Ph+ ALL)
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Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: concentration reduced by rifampicin
- avoid.
Antipsychotics: avoid concomitant use with
clozapine (increased risk of agranulocytosis).
