PD 166285
PD 166285 Basic information
- Product Name:
- PD 166285
- Synonyms:
-
- 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one Hydrochloride
- PD 166285
- PD 166285 - CAS 212391-63-4 - Calbiochem
- 6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one,dihydrochloride
- 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-onedihydrochloride
- PD 166285 dihydrochloride
- 6-(2,6-Dichloro-phenyl)-2-[4-(2-diethylaMino-ethoxy)-phenylaMino]-8-Methyl-8H-pyrido[2,3-d]pyriMidin-7-one hydrochloride
- 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimi
- CAS:
- 212391-63-4
- MF:
- C26H29Cl4N5O2
- MW:
- 585.37
- Product Categories:
-
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Protein Kinase Inhibitors and Activators
- Mol File:
- 212391-63-4.mol
PD 166285 Chemical Properties
- Melting point:
- 239-242?C
- storage temp.
- Desiccate at RT
- solubility
- DMSO, Methanol
- form
- Pale yellow solid
- color
- Yellow
- Stability:
- Hygroscopic
PD 166285 Usage And Synthesis
Chemical Properties
Yellow Solid
Uses
A broad-spectrum receptor tyrosine kinase (RTK) inhibitor which shows anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT).
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
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