212391-63-4

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;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-Dichlorophenyl)-2-[[4-[2-(diethylaMino)ethoxy]phenyl]aMino]-8-Methylpyrido[2,3-d]pyriMidin-7(8H)-one;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 NO: 212391-63-4
• Molecular Formula: C26H29Cl4N5O2
• Molecular Weight: 585.37
• Product Categories: Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators
• Mol File: 212391-63-4.mol
• Article Data: 0

Chemical Properties

• Melting Point: 239-242?C
• Appearance: /
• Storage Temp.: Desiccate at RT
• Solubility: DMSO, Methanol
• Stability: Hygroscopic
• CAS DataBase Reference: PD 166285(CAS DataBase Reference)
• NIST Chemistry Reference: PD 166285(212391-63-4)
• EPA Substance Registry System: PD 166285(212391-63-4)

Safety Data

• Hazardous Substances Data: 212391-63-4(Hazardous Substances Data)

Usage

Description

PD 166285 is a cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor with IC50 values ranging from 8.4 to 98.3 nM against various kinases, including c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ. It is a yellow solid that suppresses angiogenesis both in vitro and in vivo and effectively blocks PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations and other cellular responses. PD 166285 has been shown to have anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT).

Uses

Used in Pharmaceutical Industry:
PD 166285 is used as a broad-spectrum receptor tyrosine kinase (RTK) inhibitor for its anti-angiogenic activity and anti-tumor efficacy. It is particularly effective in combination with photodynamic therapy (PDT), making it a valuable compound in the development of cancer treatments.
Used in Cancer Research:
PD 166285 is used as a research tool to study the role of tyrosine kinases in various cellular processes, including angiogenesis and tumor growth. Its ability to inhibit multiple kinases makes it a versatile compound for investigating the underlying mechanisms of cancer progression and the potential for targeted therapies.
Used in Drug Development:
PD 166285 serves as a lead compound in the development of new drugs targeting tyrosine kinases, which are often implicated in the pathogenesis of various diseases, including cancer. Its broad-spectrum activity and potent inhibition of angiogenesis make it a promising candidate for further optimization and development into a therapeutic agent.

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.