A potent inhibitor of FGFR1
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PD 166866

Item No. 22464

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)-urea
CAS Number
192705-79-6
Molecular Formula
C20H24N6O3
Formula Weight
396.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMF:PBS(pH 7.2)(1:6): 0.14 mg/mlDMSO: 2 mg/mlEthanol: 0.1 mg/ml
λmax
232, 365 nm
SMILES
NC1=NC=C(C=C(C2=CC(OC)=CC(OC)=C2)C(NC(NC(C)(C)C)=O)=N3)C3=N1
InChi Code
InChI=1S/C20H24N6O3/c1-20(2,3)26-19(27)25-17-15(8-12-10-22-18(21)24-16(12)23-17)11-6-13(28-4)9-14(7-11)29-5/h6-10H,1-5H3,(H4,21,22,23,24,25,26,27)
InChi Key
NHJSWORVNIOXIT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    PD 166866 is a potent inhibitor of fibroblast growth factor receptor 1 (FGFR1; IC50 = 52.4 nM; Ki = 45.2 nM).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Panek, R.L., Lu, G.H., Dahring, T.K., et al. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J. Pharmacol. Exp. Ther. 286(1), 569-577 (1998).

    2. Fischer, H., Taylor, N., Allerstorfer, S., et al. Fibroblast growth factor receptor-mediated signals contribute to the malignant phenotype of non-small cell lung cancer cells: Therapeutic implications and synergism with epidermal growth factor receptor inhibition. Mol. Cancer. Ther. 7(10), 3408-3419 (2008).