Derazantinib (ARQ-087)

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
250mg	$2400	Check With Us
500mg	$3000	Check With Us
1g	$4500	Check With Us

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Cat #: V3693 CAS #: 1234356-69-4 Purity ≥ 98%

Description: Derazantinib (formerly known as ARQ 087) 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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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	468.58
Molecular Formula	C29H29FN4O
CAS No.	1234356-69-4
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 94 mg/mL (199 mM)r
	Water: <1mg/mLr
	Ethanol: <1mg/mL
SMILES Code	COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1
Synonyms	ARQ 087; ARQ087; AR-Q087

Protocol	In Vitro	In 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 Vivo	Derazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions.
	Animal model	=

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	1mg	5mg	10mg	20mg
1mM	2.1341 mL	10.6705 mL	21.3411 mL	42.6821 mL
5mM	0.4268 mL	2.1341 mL	4.2682 mL	8.5364 mL
10mM	0.2134 mL	1.0671 mL	2.1341 mL	4.2682 mL
20mM	0.1067 mL	0.5335 mL	1.0671 mL	2.1341 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

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

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

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.