AP-23464

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP22041CAS No. ：845895-51-4Purity：98%

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CAS No.	845895-51-4	Cat. No.	BCP22041
Name	AP-23464
Synonyms	AP23464; AP 23464;
SMILES	CP(=O)(C)C1=CC=C(C=C1)NC2=NC(=NC3=C2N=CN3CCC4=CC(=CC=C4)O)C5CCCC5
Chemical Name
Formula	C26H30N5O4P	M. Wt	475.52
Purity	98%	Storage	Store at 4-8°C
Description	AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the low nanomolar cellular and biochemical inhibitory properties of AP23464 extend to frequently observed imatinib mesylate-resistant Bcr-Abl mutants, including nucleotide binding P-loop mutants Q252H, Y253F, E255K, C-terminal loop mutant M351T, and activation loop mutant H396P. AP23464 was ineffective against mutant T315I, an imatinib mesylate contact residue. The potency of AP23464 against imatinib mesylate-refractory Bcr-Abl and its distinct binding mode relative to imatinib mesylate warrant further investigation of AP23464 for the treatment of CML.