A potent inhibitor of FGFR1 (IC50 = 52.4 nM; Ki = 45.2 nM); selective for FGFR1 over PDGFR

PD 166866 – 10 mg

Brand:
Cayman
CAS:
192705-79-6
Storage:
-20
UN-No:
Non-Hazardous - /

PD 166866 is a potent inhibitor of fibroblast growth factor receptor 1 (FGFR1; IC50 = 52.4 nM; Ki = 45.2 nM).{40429} It is selective for FGFR1 over PDGFR, EGFR, C-SRC, MEK, PKC, insulin receptor tyrosine kinase, and CDK4 (IC50s = >50 μM). PD 166866 inhibits FGFR1 autophosphorylation in NIH3T3 and L6 cells (IC50s = 10.8 and 3.1 nM, respectively) and inhibits phosphorylation of MAPK (IC50s = 4.3 and 7.9 nM for the 44- and 42-kDa MAPK isoforms, respectively). It reduces FGF- but not EGF- or PDGF-stimulated growth of L6 cells and inhibits microvessel outgrowth from human placental arteries in vitro. PD 166866 inhibits the growth of non-small cell lung cancer (NSCLC) cell lines in a dose-dependent manner and reduces migration of VL-8 cells at a concentration of 10 μM.{40430}  

 

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Description

A potent inhibitor of FGFR1 (IC50 = 52.4 nM; Ki = 45.2 nM); selective for FGFR1 over PDGFR, EGFR, C-SRC, MEK, PKC, insulin receptor tyrosine kinase, and CDK4 (IC50s = >50 μM); inhibits FGFR1 autophosphorylation in NIH3T3 and L6 cells (IC50s = 10.8 and 3.1 nM, respectively); inhibits phosphorylation of MAPK (IC50 = 4.3 and 7.9 nM for the 44- and 42-kDa MAPK isoforms, respectively); reduces FGF- but not EGF- or PDGF-stimulated growth of L6 cells and inhibits microvessel outgrowth from human placental arteries in vitro; inhibits growth of NSCLC cell lines a dose-dependent manner; reduces migration of VL-8 cells at a concentration of 10 μM

Formal name: N-[2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N’-(1,1-dimethylethyl)-urea

Synonyms: 

Molecular weight: 396.4

CAS: 192705-79-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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