PD166866

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PD166866
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Cat #: V2723 CAS #: 192705-79-6 Purity ≥ 98%

Description: PD166866, a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines, is a a new nanomolar potent and selective small molecule inhibitor of FGFR (fibroblast growth factor-1 receptor) tyrosine kinase inhibitor with an IC50 of 52.4 nM.

References: Panek RL, 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. 1998 Jul;286(1):569-77.

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Molecular Weight (MW)396.44
Molecular FormulaC20H24N6O3
CAS No.192705-79-6
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 14 mg/mL (35.3 mM)r
Water: <1 mg/mLr
Ethanol: 3 mg/mL (7.6 mM)
SMILES CodeN#CC1=CC=C(C(N=C(N2CCC(N)CC2)N3C)=C(C4=CC=C(OC)C(F)=C4)C3=O)C=C1F.O=S(C5=CC=CC=C5)(O)=O
SynonymsPD166866; PD166866; PD 166866
ProtocolIn VitroPD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 nM and is characterized as an ATP competitive inhibitor of the FGFR-1. PD 166866 is a potent inhibitor of FGFR autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase. PD 166866 also inhibits bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells. Daily exposure of PD 166866 to L6 cells at concentrations from 1 to 100 nM results in a concentration-related inhibition of bFGF-stimulated cell growth for 8 consecutive days with an IC50 value of 24 nM.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5224 mL12.6122 mL25.2245 mL50.4490 mL
5mM0.5045 mL2.5224 mL5.0449 mL10.0898 mL
10mM0.2522 mL1.2612 mL2.5224 mL5.0449 mL
20mM0.1261 mL0.6306 mL1.2612 mL2.5224 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Volume(final)
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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.