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

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

Cat. No.: HY-15729A Purity: 97.45%
Handling Instructions

Rociletinib hydrobromide (CO-1686 hydrobromide) 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.

Rociletinib hydrobromide Chemical Structure

Rociletinib hydrobromide Chemical Structure

CAS No. : 1446700-26-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
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100 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Rociletinib hydrobromide:

Top Publications Citing Use of Products

    Rociletinib hydrobromide purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2020 Jan.

    Rociletinib enhances the anticancer effect of topotecan in the S1-MI-80 tumor xenograft model in nude mice. (A)The changes in tumor volume over time after the S1-MI-80 cell implantation (n=6). Data shown are mean±SD of tumor volumes for each group. (B) The image of tumors size in four groups excised from the mice on the 75th day after implantation.

    Rociletinib hydrobromide purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2020 Jan.

    The protein level of ABCG2 on MDR cells after 0, 0.25, 0.5 and 1 µmol/L rociletinib stimulation for 48 h are measured by Western blot analysis.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rociletinib hydrobromide (CO-1686 hydrobromide) 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[1]

    EGFRL858R/T790M

    21.5 nM (Ki)

    EGFRT790M

    303.3 nM (Ki)

    In Vitro

    Rociletinib (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[1].

    In Vivo

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

    Clinical Trial
    Molecular Weight

    636.46

    Formula

    C₂₇H₂₉BrF₃N₇O₃

    CAS No.

    1446700-26-0

    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.[H]Br

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 59 mg/mL (92.70 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5712 mL 7.8560 mL 15.7119 mL
    5 mM 0.3142 mL 1.5712 mL 3.1424 mL
    10 mM 0.1571 mL 0.7856 mL 1.5712 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (3.93 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    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 (Rociletinib) 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 (Rociletinib) as outlined (N=10 animals/gp). The LUM1686 PDX xenograft study is performed by CrownBio. Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib) 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
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    Keywords:

    RociletinibCO-1686AVL-301CNX-419CO1686CO 1686AVL301AVL 301CNX419CNX 419EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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    Product Name:
    Rociletinib hydrobromide
    Cat. No.:
    HY-15729A
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