AP24534 (Ponatinib)

Catalog No. A10080

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。

Product Citations

Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
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

Technical details

Catalog Num	A10080
M. Wt	532.6
Formula	C29H27F3N6O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	943319-70-8
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

Biological Activity

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。

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

Solubility *

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.

Preparing Stock Solutions

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.