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

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0551
    CAS #: 1374640-70-6Purity ≥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. It inhibits EGFRL858R/T790M and EGFRWT with Ki values of 21.5 nM and 303.3 nM in cell-free assays, respectively. Rociletinib shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy by binding to and inhibiting mutant forms of EGFR such as T790M, thus leading to cell death of resistant tumor cells. 

    References: Cancer Discov. 2013 Dec;3(12):1404-15.

    Related CAS No.: 1374640-70-6 (free base)  1446700-26-0 (HBr)

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    Molecular Weight (MW)555.55
    FormulaC27H28F3N7O3
    CAS No.1374640-70-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (180.0 mM)
    Water: <1 mg/mL
    Ethanol: 55 mg/mL (202.0 mM)
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL 
    Synonyms

    Synonym: Rociletinib; AVL301; CO 1686; AVL 301; CNX419; AVL-301; CO1686; CO-1686; CNX 419; CNX-419.

    Chemical Name: N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide

    InChi Key: HUFOZJXAKZVRNJ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35)

    SMILES Code: C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O


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    In Vitro

    In vitro activity: CO-1686 inhibits p-EGFR with IC50 ranging from 62 to 187 nM in the mutant EGFR–expressing cells, while inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. CO-1686 selectively inhibits growth of NSCLC cells expressing mutant EGFR with GI50 ranging from 7 to 32 nM, and induces apoptosis. CO-1686–resistant NSCLC cell lines exhibits signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors.


    Kinase Assay: Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor. 


    Cell Assay: Cells [NSCLC cell lines expressing mutant EGFR (HCC827, PC9, HCC827-EPR, and NCI-H1975) and cell lines expressing WT EGFR (A431, NCI-H1299, and NCI-H358)] are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.

    In VivoCO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
    Animal modelHuman EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
    Formulation & DosageDissolved in DMSO: Solutol HS15: PBS (5:15:80; v:v:v);  50 mg/kg; Oral gavage
    References

    Cancer Discov. 2013 Dec;3(12):1404-15.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Rociletinib (CO-1686, AVL-301)

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


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