PD 166285 dihydrochloride - CAS 212391-63-4
Category: Inhibitor
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PD 166285, a novel protein tyrosine kinase inhibitor of a new structural class, is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1), and PDGFRβ (platelet-derived growth factor receptor β) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). PD 166285 also inhibits the checkpoint kinases Wee1 and MYT1 (Myt1), abolishes Cdc2 phosphorylation in numerous tumor cell lines, and abrogates the G2 checkpoint.
≥99% by HPLC
Yellow solid
PD 166285 dihydrochloride; PD166285 dihydrochloride; PD-166285 dihydrochloride6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one dihydrochloride
DMSO to 100 mM
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.American Association for Cancer Research 1999: 10-14 April, Philadelphia, Pennsylvania.
Lavelle F1. Expert Opin Investig Drugs. 1999 Jun;8(6):903-9.
No genuinely new targets or drugs were disclosed; instead, data about known therapeutic approaches and compounds were consolidated. The results of Phase I clinical trials were presented for the two farnesyl transferase inhibitors R 115777 and L 778,123. These results will certainly contribute to the debate concerning the best way to use signal transduction inhibitors in clinic. It will take many years to appreciate fully the clinical potential of such compounds. Many preclinical presentations were given on the subject of new tyrosine protein kinases inhibitors for the treatment of angiogenesis, with the target kinases being the epidermal growth factor receptor (EGF-R) family, cyclin-dependent kinases (CDKs) and vascular endothelial growth factor receptor (VEGF-R). Inhibitors with convincing in vivo antitumour activity belong exclusively to three chemical series, quinazolines, indolinones and pyrido-pyrimidines. Among these series, the principal new compounds are ZD 1490, PD 183805, PD 166285, SU 6668 and GW 5181.
2.Entry into a new class of protein kinase inhibitors by pseudo ring design.
Furet P1, Caravatti G, Guagnano V, Lang M, Meyer T, Schoepfer J. Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.
A pyrimidin-4-yl-urea motif forming a pseudo ring by intramolecular hydrogen bonding has been designed to mimic the pyrido[2,3-d]pyrimidin-7-one core structure of a well-established class of protein kinase inhibitors. Potent inhibition of a number of protein kinases was obtained with the first prototype compound synthesized to probe the design concept.
3.Therapeutic targeting of Src-kinase Lyn in myeloid leukemic cell growth.
Roginskaya V1, Zuo S, Caudell E, Nambudiri G, Kraker AJ, Corey SJ. Leukemia. 1999 Jun;13(6):855-61.
Protein tyrosine kinases play a major role in promoting cell growth, and their activity in solid tumors is well established. Inhibitors of protein tyrosine kinases are now in advanced clinical trials for the treatment of breast and brain cancers. Because Src-related PTK have been shown to be activated in leukemic cell lines, we studied their activation in human myeloid leukemia. Blasts from the majority of patients with acute leukemia showed constitutive activity of the Src kinase Lyn. In contrast, no patient samples showed constitutive activation of Jak2. Genetic and pharmacologic targeting of Lyn was used to determine its contribution to leukemic cell growth. Antisense Lyn oligonucleotide treatment resulted in the inhibition of tritiated thymidine incorporation following GM-CSF stimulation of the factor-dependent line MO7e. The Src kinase inhibitor PD166285 inhibited the growth of human leukemic cell lines and leukemic blasts. When combined with doxorubicin, an additive effect on the inhibition of leukemic cell growth occurred.
4.In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.
Panek RL1, Lu GH, Klutchko SR, Batley BL, Dahring TK, Hamby JM, Hallak H, Doherty AM, Keiser JA. J Pharmacol Exp Ther. 1997 Dec;283(3):1433-44.
PD 166285, a novel protein tyrosine kinase inhibitor of a new structural class, the 6-aryl-pyrido[2,3-d]pyrimidines, was synthesized as the most potent and soluble analog of a series of small molecules originally identified by screening a compound library with assays that measured protein tyrosine kinase activity. PD 166285 was found to inhibit Src nonreceptor tyrosine kinase, fibroblast growth factor receptor-1, epidermal growth factor receptor and platelet-derived growth factor receptor beta subunit (PDGFR-beta), tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 8.4 +/- 2.3 nM (n = 6), 39.3 +/- 2.8 nM (n = 16), 87.5 +/- 13.7 nM (n = 6) and 98.3 +/- 7.9 nM (n = 16), respectively. PD 166285 also demonstrated inhibitory activity against mitogen-activated protein kinase (IC50 = 5 microM) and protein kinase C (IC50 = 22.7 microM). PD 166285 was further characterized as an ATP competitive inhibitor of Src nonreceptor tyrosine kinase, PDGFR-beta, fibroblast growth factor receptor-1 and epidermal growth factor receptor tyrosine kinases.
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CAS 212391-63-4 PD 166285 dihydrochloride

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