WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406170
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.
MedKoo Cat#: 406170
Chemical Formula: C24H34N5OP
Exact Mass: 439.2501
Molecular Weight: 439.53
Elemental 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
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, Gallick GE, Sood AK. Antiangiogenic and antitumor effects of SRC inhibition in ovarian 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, Dalgarno DC, Sawyer TK, Daley GQ. Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci 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, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther. 2005 Dec;4(12):1900-11. PubMed PMID: 16373705.