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Crenolanib (CP-868596; RO 002; ARO 002)

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Crenolanib (CP-868596; RO 002; ARO 002)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1060Check With Us
500mg$1650Check With Us
1g$2475Check With Us

Cat #: V0580 CAS #: 670220-88-9 Purity ≥ 98%

Description: Crenolanib (formerly also known as CP868596; RO-002; ARO-002), a benzimidazole compound, is an orally bioavailable and selective small molecule inhibitor of platelet-derived growth factor receptor (PDGFRα/β) with potential anticancer activity.

References: Heinrich MC, et al.Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with STI571-resistant gastrointestinal stromal tumors. Clin Cancer Res, 2012, Jun 27.

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Molecular Weight (MW)443.54
Molecular FormulaC26H29N5O2
CAS No.670220-88-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 89 mg/mL (200.6 mM)r
Water:<1 mg/mLr
Ethanol: 7 mg/mL (15.8 mM)
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES CodeNC1CCN(C2=C3N=C(N4C=NC5=CC(OCC6(C)COC6)=CC=C45)C=CC3=CC=C2)CC1
SynonymsRO 002; ARO 002, CP-868596; ARO-002; CP 868596; CP868596; ARO002; RO-002; RO002
ProtocolIn VitroCrenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC50 values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC50 values of 93 and 26 nM, respectively.
In VivoCrenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice.
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
1mM2.2546 mL11.2729 mL22.5459 mL45.0918 mL
5mM0.4509 mL2.2546 mL4.5092 mL9.0184 mL
10mM0.2255 mL1.1273 mL2.2546 mL4.5092 mL
20mM0.1127 mL0.5636 mL1.1273 mL2.2546 mL
Quality Control Documentation
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)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
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.