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Birabresib (Synonyms: OTX-015; MK-8628)

Cat. No.: HY-15743 Purity: 99.81%
Handling Instructions

Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.

For research use only. We do not sell to patients.

Birabresib Chemical Structure

Birabresib Chemical Structure

CAS No. : 202590-98-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
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100 mg USD 504 In-stock
Estimated Time of Arrival: December 31
200 mg USD 960 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Birabresib purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 May;10(5). pii: e8446.

    NRAS-mutant melanoma cells grown as collagen-embedded 3D spheroids are treated with DMSO, 0.1 μM MEKi PD901, 0.5 μM BETi (JQ-1 or OTX-015), or BETi+MEKi combination for 5 days. Spheroids are stained with Calcein (AM) (green; live cells) and EtBr (red; dead cells) and imaged using a fluorescence microscope.

    Birabresib purchased from MCE. Usage Cited in: Cancer Res. 2019 May 15;79(10):2761-2774.

    BETi dampens signaling downstream of receptor tyrosine kinases. Western blotting of HER3 and downstream effectors in response to increasing doses of OTX015 at 24h. SCCOHT1, OVK18: SCCOHT cells; OVCAR8, SKOV3, and IGROV1, serous ovarian carcinoma cells.

    Birabresib purchased from MCE. Usage Cited in: Cancer Res. 2019 May 15;79(10):2761-2774.

    Western blot analysis of HER3 in SCCOHT1 cells after re-expression and dose-dependent treatment with OTX015 at 24h.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.

    IC50 & Target

    IC50: 92-112 nM (BRD2, BRD3, BRD4)[1]

    In Vitro

    Birabresib (OTX-015) (500 nM) exposure induces a strong decrease of BRD2, BRD4 and c-MYC and increase of HEXIM1 proteins, while BRD3 expression is unchanged. c-MYC, BRD2, BRD3, BRD4 and HEXIM1 mRNA levels do correlate however with viability following exposure to Birabresib (OTX-015)[2]. Birabresib (OTX-015) (0.1, 1, 5 μM) treatment induces HIV-1 full-length transcripts and viral outgrowth in resting CD4+ T cells from infected individuals receiving suppressive antiretroviral therapy (ART), while exerting minimal toxicity and effects on T cell activation. Birabresib-mediated activation of HIV-1 involves an increase in CDK9 occupancy and RNAP II C-terminal domain (CTD) phosphorylation[3].

    In Vivo

    In MDA-MB-231 murine xenografts, tumor mass is significantly (p < 0.05) reduced by Birabresib (OTX-015) (50 mg/kg) with respect to vehicle-treated animals. Birabresib (OTX-015) in combination with 2 mg/kg RAD001 shows more effective activity than Birabresib alone[4].

    Clinical Trial
    Molecular Weight

    491.99

    Formula

    C₂₅H₂₂ClN₅O₂S

    CAS No.

    202590-98-5

    SMILES

    O=C(NC1=CC=C(O)C=C1)C[[email protected]]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2

    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 : ≥ 49 mg/mL (99.60 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 2.0326 mL 10.1628 mL 20.3256 mL
    5 mM 0.4065 mL 2.0326 mL 4.0651 mL
    10 mM 0.2033 mL 1.0163 mL 2.0326 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 (5.08 mM); Clear solution

    • 2.

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

      Solubility: 2.5 mg/mL (5.08 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    For the MTT assay, cells are seeded in 24-well plates at 1×106 per well and treated with Birabresib (OTX-015) (0.01 nM-10 μM) for 72 h. Cells are transferred to 96-well plates and incubated with 0.5 mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) in the dark at 37°C for 4 h. Cells are then lysed with 25% sodium dodecyl sulfate (SDS) lysis buffer and absorbance is read at 570 nm using a Microplate Reader. Three independent experiments are run for each cell line and untreated cells are used as negative controls.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Mice are subcutaneously injected in the right flank with 10×106 MDA-MB-231 cells. When average tumor weight is appr 130 mg, mice are randomized (nine animals/group) to one of the following experimental groups: vehicle (for Birabresib (OTX-015), water, twice daily, oral; for RAD001 vehicle, 5% Tween-80/5% polyethylene glycol 400, thrice weekly, intraperitoneal); 50 mg/kg Birabresib (OTX-015), twice daily, oral; 2 mg/kg RAD001, thrice weekly, intraperitoneal; 50 mg/kg Birabresib (OTX-015) + 2 mg/kg RAD001, according to the single agent dosing schedules.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.81%

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    Product Name:
    Birabresib
    Cat. No.:
    HY-15743
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