1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

CO-1686 (Synonyms: Rociletinib; AVL-301; CNX-419)

Cat. No.: HY-15729 Purity: 98.45%
Handling Instructions

CO-1686 is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

For research use only. We do not sell to patients.
CO-1686 Chemical Structure

CO-1686 Chemical Structure

CAS No. : 1374640-70-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 73 In-stock
5 mg USD 60 In-stock
10 mg USD 96 In-stock
50 mg USD 198 In-stock
100 mg USD 306 In-stock
200 mg USD 480 In-stock
500 mg USD 660 In-stock
1 g   Get quote  
5 g   Get quote  

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Customer Review

Other Forms of CO-1686:

    CO-1686 purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    CO-1686 purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

    CO-1686 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of Ibrutinib on EGFR wt/mutant NSCLCs. Ibrutinib effects on wt EGFR and mutant EGFR- mediated signaling pathways. The results demonstrate that Ibrutinib potently inhibits both EGFR wt/mutant auto-phosphorylation at Y1068.

    CO-1686 purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of Ibrutinib, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

    CO-1686 purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 25;7(43):69760-69769.

    Ibrutinib and WZ4002 inhibitory effects on EGFRY1068 auto-phosphorylation in the H1975 cell line at different time points by removal of drug after 4 h pretreatment

    CO-1686 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Dec 13. pii: molcanther.0324.2017.

    Immunoblot analysis of U-CH1, MUG-Chor1 and Chor-IN-1 cells treated with Afatinib for 2 h or 48 h. Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s for each cell line are reported.

    CO-1686 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Dec 13. pii: molcanther.0324.2017.

    Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s of the different inhibitors are reported.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    CO-1686 is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

    IC50 & Target

    Ki: 21.5 nM (EGFRL858R/T790M), 303.3 nM (EGFR)

    In Vitro

    CO-1686 (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. CO-1686 potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. CO-1686 resistant NSCLC cell lines are sensitive to AKT inhibition[1].

    In Vivo

    CO-1686 (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. CO-1686 (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.8000 mL 9.0001 mL 18.0002 mL
    5 mM 0.3600 mL 1.8000 mL 3.6000 mL
    10 mM 0.1800 mL 0.9000 mL 1.8000 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    CO-1686 is dissolved in DMSO.

    Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (CO-1686) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI50) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×107 tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm3, Animals are dosed with compounds (CO-1686) as outlined (N=10 animals/gp). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (CO-1686) is initiated at a mean tumor size of approximately 160 mm3. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm3. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    555.55

    Formula

    C₂₇H₂₈F₃N₇O₃

    CAS No.

    1374640-70-6

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 43 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.45%

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    Inquiry Information

    Product Name:
    CO-1686
    Cat. No.:
    HY-15729
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