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Rociletinib (CO-1686, AVL-301, CNX-419)

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

Rociletinib (CO-1686, AVL-301, CNX-419)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
500mg$630Check With Us
1g$850Check With Us
5g$2150Check With Us

Cat #: V0551 CAS #: 1374640-70-6 Purity ≥ 98%

Description: Rociletinib (formerly CO1686; AVL301; CNX419) is an orally bioavailable, covalent / irreversible, and mutant-selective EGFR (e.g. T790M) inhibitor with potential antineoplastic activity.

References: Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

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Product Promise

Promise
Molecular Weight (MW)555.55
Molecular FormulaC27H28F3N7O3
CAS No.1374640-70-6
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 100 mg/mL (180.0 mM)r
Water: <1 mg/mLr
Ethanol: 55 mg/mL (202.0 mM)
Solubility In Vivo1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
SMILES CodeC=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
SynonymsRociletinib; AVL301; CO 1686; AVL 301; CNX419; AVL-301; CO1686; CO-1686; CNX 419; CNX-419
ProtocolIn VitroRociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition.
In VivoRociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic 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
1mM1.8000 mL9.0001 mL18.0002 mL36.0004 mL
5mM0.3600 mL1.8000 mL3.6000 mL7.2001 mL
10mM0.1800 mL0.9000 mL1.8000 mL3.6000 mL
20mM0.0900 mL0.4500 mL0.9000 mL1.8000 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.