WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406173
Description: PD166326 is one of the most potent members of the pyridopyrimidine class of protein tyrosine kinase inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl kinase activity after a single oral dose and demonstrated marked antileukemic activity in vivo. In vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.
MedKoo Cat#: 406173
Chemical Formula: C21H16Cl2N4O2
Exact Mass: 426.06503
Molecular Weight: 427.28334
Elemental Analysis: C, 59.03; H, 3.77; Cl, 16.59; N, 13.11; O, 7.49
Synonym: PD166326; PD166326; PD 166326.
IUPAC/Chemical Name: 6-(2,6-dichlorophenyl)-2-((3-(hydroxymethyl)phenyl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
InChi Key: ZIQFYVPVJZEOFS-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H16Cl2N4O2/c1-27-19-13(9-15(20(27)29)18-16(22)6-3-7-17(18)23)10-24-21(26-19)25-14-5-2-4-12(8-14)11-28/h2-10,28H,11H2,1H3,(H,24,25,26)
SMILES Code: O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(CO)=C4)N=C3N1C
1: Grosso S, Puissant A, Dufies M, Colosetti P, Jacquel A, Lebrigand K, Barbry P, Deckert M, Cassuto JP, Mari B, Auberger P. Gene expression profiling of imatinib and PD166326-resistant CML cell lines identifies Fyn as a gene associated with resistance to BCR-ABL inhibitors. Mol Cancer Ther. 2009 Jul;8(7):1924-33. doi: 10.1158/1535-7163.MCT-09-0168. Epub 2009 Jun 30. PubMed PMID: 19567819.
2: Wolff NC, Veach DR, Tong WP, Bornmann WG, Clarkson B, Ilaria RL Jr. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003. Epub 2005 Jan 18. PubMed PMID: 15657179; PubMed Central PMCID: PMC1895078.
3: von Bubnoff N, Veach DR, van der Kuip H, Aulitzky WE, SÃ¤nger J, Seipel P, Bornmann WG, Peschel C, Clarkson B, Duyster J. A cell-based screen for resistance of Bcr-Abl-positive leukemia identifies the mutation pattern for PD166326, an alternative Abl kinase inhibitor. Blood. 2005 Feb 15;105(4):1652-9. Epub 2004 Sep 30. PubMed PMID: 15459011.