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Derazantinib racemate

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Derazantinib racemate
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Cat #: V3694 CAS #: 1234356-69-4 (R-enantiomer) Purity ≥ 98%

Description: Derazantinib Racemate is the racemic mixture of derazantinib which is formerly known as ARQ 087 and is a novel, orally bioavailable, ATP competitive, small molecule, multi-kinase inhibitor with potent in vitro and in vivo activity against FGFR (fibroblast growth factor receptor) addicted cell lines and tumors with IC50s of 4.5, 1.8, and 4.5 nM for FGFR1-3 respectively in biochemical assay, IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3.

References: Hall TG, et al. Preclinical Activity of ARQ-087, a Novel Inhibitor Targeting FGFR Dysregulation. PLoS One. 2016 Sep 14;11(9):e0162594.

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Molecular Weight (MW)468.58
Molecular FormulaC29H29FN4O
CAS No.1234356-69-4 (R-enantiomer)
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 94 mg/mL (199 mM)r
Water: <1mg/mLr
Ethanol: <1mg/mL
SMILES CodeCOCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1
SynonymsARQ 087; ARQ087; AR-Q087 racemate
ProtocolIn VitroIn cells, inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) is evident by the response to Derazantinib treatment. Cell proliferation studies demonstrate Derazantinib has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein show a positive relationship between Derazantinib induced G1 cell cycle arrest and subsequent induction of apoptosis.
In VivoDerazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions.
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
1mM2.1341 mL10.6705 mL21.3411 mL42.6821 mL
5mM0.4268 mL2.1341 mL4.2682 mL8.5364 mL
10mM0.2134 mL1.0671 mL2.1341 mL4.2682 mL
20mM0.1067 mL0.5335 mL1.0671 mL2.1341 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
 
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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

Concentration(start)
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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.