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HomeProduct name listPD 166285

PD 166285

Synonym(s):PD 166285 - CAS 212391-63-4 - Calbiochem;PD166285, PD0166285, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, PDGFR Tyrosine Kinase Inhibitor XIX, Wee1 Inhibitor IV;PDGFR Tyrosine Kinase Inhibitor XIX, Wee1 Inhibitor IV, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, PD166285, PD0166285

PD 166285 Structural

What is PD 166285?

Chemical properties

Yellow Solid

The Uses of PD 166285

A broad-spectrum receptor tyrosine kinase (RTK) inhibitor which shows anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT).

What are the applications of Application

PD 166285 is an inhibitor of RTK, c-Src, FGFR1, Wee 1, and PDGFRβ

General Description

A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC50 against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC50 = 3.4, 5, and 22.7 μM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 μM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC50 = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.

Biological Activity

Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFR β ) (IC 50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G 2 checkpoint.

storage

Desiccate at RT

Properties of PD 166285

Melting point: 239-242?C
storage temp.  Desiccate at RT
solubility  DMSO, Methanol
form  Pale yellow solid
color  Yellow
Stability: Hygroscopic

Safety information for PD 166285

Computed Descriptors for PD 166285

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