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    Icotinib (BPI2009)
    Icotinib (BPI2009)

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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 #: V0569
    CAS #: 610798-31-7 Purity ≥98%

    Description: Icotinib (formerly known as BPI-2009; trade name Conmana), a side chain-cyclized form of erlotinib, is an orally available and specific EGFR inhibitor with potent anticancer activity. Icotinib is structurally similar to erlotinib and was approved in China to treat lung cancer (NSCLC) in 2011. It inhibits EGFR with an IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). When profiled with 88 kinases, Icotinib only showed meaningful inhibitory activity to EGFR and its mutants. Icotinib blocked EGFR-mediated intracellular tyrosine phosphorylation (IC50 = 45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation. In vivo studies demonstrated that Icotinib exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug was well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780). The data shows that Icotinib was non-inferior to Gefitinib in terms of median progression free survival (PFS) and safety superior favor to Icotinib compared to Gefitinib.

    ReferencesLung Cancer. 2012 May;76(2):177-82.

    Related CAS: 610798-31-7 (free base); 1204313-51-8 (HCl)

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    Molecular Weight (MW)391.42
    FormulaC22H21N3O4
    CAS No.610798-31-7 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 78 mg/mL (199.2 mM)
    Water: <1 mg/mL
    Ethanol: 7 mg/mL (17.88 mM)
    Solubility (In vivo)0.5% CMC: 30mg/mL
    SynonymsBPI-2009; BPI2009; BPI 2009; BPI2009H; BPI-2009H; BPI 2009H; Icotinib; Trade name: Conmana. 

    Chemical Name: N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride

    InChi Key: PNNGXMJMUUJHAV-UHFFFAOYSA-N

    InChi Code: InChI=1S/C22H21N3O4.ClH/c1-2-16-4-3-5-17(12-16)25-22-18-13-20-21(14-19(18)23-15-24-22)29-11-9-27-7-6-26-8-10-28-20;/h1,3-5,12-15H,6-11H2,(H,23,24,25);1H

    SMILES Code: C#CC1=CC(NC2=C3C=C(OCCOCCOCCO4)C4=CC3=NC=N2)=CC=C1.[H]Cl


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    In Vitro

    In vitro activity: Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR.


    Kinase Assay: In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi 32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30 °C for 20 min. After quenching with SDS sample buffer at 100 °C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to the PhosphorImager to detect radioactivity. Quantification is performed by ImageQuant software. In this methodology the radioactive signal inversely correlates with kinase activity.


    Cell Assay:  Cells (103 /well, A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cells.) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 °C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4.

    In VivoIcotinib shows an antitumor effect in different types of xenografts. Icotinib inhibits tumor growth at a rate of 51.5%, 31.0% and 67.4% in the A431, A549 and H460 xenografts at a dose of 120 mg/kg, respectively.
    Animal modelNude mice bearing A431, A549, H460 and HCT8 cells
    Formulation & Dosage Dissolved in 0.5% CMC-Na.; 30, 60, 120 mg/kg; p.o.
    References

    Lung Cancer. 2012 May;76(2):177-82.


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

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