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$0.00 - Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
Biological Activity
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
Targets
| Target | Value |
|---|---|
| Abl | IC50: 0.37nM |
| PDGFRα | IC50: 1.1nM |
| VEGFR2 | IC50: 1.5nM |
| FGFR1 | IC50: 2.2nM |
| c-Src | IC50: 5.4nM |
| c-Kit | IC50: 12.5nM |
| Insulin Receptor | IC50: >1μM |
| IGF-1R | IC50: >1μM |
| AuroraA | IC50: >1μM |
| CDK2/CyclinE | IC50: >1μM |
| In vitro (25°C) | DMSO | 30 mg/mL (56.33 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1% CMC Na | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.78 mL | 93.88 mL | 187.76 mL |
| 0.5 mM | 3.76 mL | 18.78 mL | 37.55 mL |
| 1 mM | 1.88 mL | 9.39 mL | 18.78 mL |
| 5 mM | 0.38 mL | 1.88 mL | 3.76 mL |
*The above data is based on the productmolecular weight 532.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10080 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 943319-70-8 |
| Formula | C29H27F3N6O |
| M. Wt | 532.6 |
| Purity | >98% |
| Synonyms | Ponatinib |
| SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CN=C5N4N=CC=C5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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