AP23846

WARNING: This product is for research use only, not for human or veterinary use.

Description:AP23846 is a potent c-Src kinase inhibitor (IC50 approximately 0.5 nmol/L in vitro, approximately 10-fold more potent than PP2, the most widely used commercially available Src family kinase inhibitor). At concentrations of 1 micromol/L, AP23846 led to complete Src inhibition for 48 hours in cells. No cytotoxicity was observed under these conditions, although proliferation rates were slower. Therefore, this was an excellent inhibitor to examine Src-regulated signaling pathways in tumor cells. AP23846 reduced cellular migration, vascular endothelial growth factor, and interleukin-8 in a dose-dependent fashion in pancreatic adenocarcinoma cells grown in vitro.

Price and Availability

AP23846, purity > 98%, is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406170Name: AP23846CAS#: 878654-51-4Chemical Formula: C24H34N5OPExact Mass: 439.2501Molecular Weight: 439.53Elemental Analysis: C, 65.58; H, 7.80; N, 15.93; O, 3.64; P, 7.05

Synonym:AP23846; AP 23846; AP-23846

IUPAC/Chemical Name:(4-((2-cyclopentyl-9-ethyl-9H-purin-6-yl)amino)phenyl)dipropylphosphine oxide

InChi Key:QWYGJEVWFGFNRP-UHFFFAOYSA-N

InChi Code:InChI=1S/C24H34N5OP/c1-4-15-31(30,16-5-2)20-13-11-19(12-14-20)26-23-21-24(29(6-3)17-25-21)28-22(27-23)18-9-7-8-10-18/h11-14,17-18H,4-10,15-16H2,1-3H3,(H,26,27,28)

SMILES Code:CCCP(CCC)(C1=CC=C(NC2=C3N=CN(CC)C3=NC(C4CCCC4)=N2)C=C1)=O

Technical Data

Additional Information

References

1: Han LY, Landen CN, Trevino JG, Halder J, Lin YG,Kamat AA, Kim TJ, Merritt WM, Coleman RL, Gershenson DM, Shakespeare WC,Wang Y, Sundaramoorth R, Metcalf CA 3rd, Dalgarno DC, Sawyer TK, GallickGE, Sood AK. Antiangiogenic and antitumor effects of SRC inhibition inovarian carcinoma. Cancer Res. 2006 Sep 1;66(17):8633-9. PubMed PMID:16951177; PubMed Central PMCID: PMC3202609.

2: Azam M, Nardi V, Shakespeare WC, Metcalf CA 3rd, Bohacek RS, Wang Y,Sundaramoorthi R, Sliz P, Veach DR, Bornmann WG, Clarkson B, DalgarnoDC, Sawyer TK, Daley GQ. Activity of dual SRC-ABL inhibitors highlightsthe role of BCR/ABL kinase dynamics in drug resistance. Proc Natl AcadSci U S A. 2006 Jun 13;103(24):9244-9. Epub 2006 Jun 5. PubMed PMID:16754879; PubMed Central PMCID: PMC1482597.

3: Summy JM, Trevino JG, Lesslie DP, Baker CH, Shakespeare WC, Wang Y,Sundaramoorthi R, Metcalf CA 3rd, Keats JA, Sawyer TK, Gallick GE.AP23846, a novel and highly potent Src family kinase inhibitor, reducesvascular endothelial growth factor and interleukin-8 expression in humansolid tumor cell lines and abrogates downstream angiogenic processes.Mol Cancer Ther. 2005 Dec;4(12):1900-11. PubMed PMID: 16373705.