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

Name: Birabresib
Brand: MedChemExpress
SKU: HY-15743
Rating: 5.0 (32 reviews)

Cat. No.: HY-15743 Purity: 99.75%: FAQs
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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

CAS No. : 202590-98-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 32 publication(s) in Google Scholar

Other Forms of Birabresib:

(R)-Birabresib Get quote
Birabresib (Standard) Get quote

29 Publications Citing Use of MCE Birabresib

: Birabresib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2019 May 15;79(10):2761-2774. [Abstract]; 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 MedChemExpress. Usage Cited in: Cancer Res. 2019 May 15;79(10):2761-2774. [Abstract]; Western blot analysis of HER3 in SCCOHT1 cells after re-expression and dose-dependent treatment with OTX015 at 24h.

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

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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]

Cellular Effect

Cell Line	Type	Value	Description	References
CAKI-1	GI₅₀	94.6 nM Compound: OTX-015	Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
Daoy	GI₅₀	160 nM Compound: OTX-015; MK-8628	Antitumor activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antitumor activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 33636537]
HAL-01	IC₅₀	2.53 μM Compound: OTX-015	Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
HCT-15	GI₅₀	178.6 nM Compound: OTX-015	Antiproliferative activity against human HCT-15 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT-15 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
HL-60	IC₅₀	0.82 μM Compound: OTX-015	Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
HL-60(TB)	GI₅₀	178.6 nM Compound: OTX-015	Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
HPBALL	IC₅₀	7.01 μM Compound: OTX-015	Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
K562	IC₅₀	2.84 μM Compound: OTX-015	Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
Kasumi 1	IC₅₀	135 nM Compound: 4; OTX-015	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MDA-MB-468	GI₅₀	212.3 nM Compound: OTX-015	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
MM1.S	IC₅₀	137 nM Compound: 4; OTX-015	Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MM1.S	IC₅₀	22.7 nM Compound: 2; OTX015	Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay	[PMID: 31461688]
MM1.S	IC₅₀	6.3 nM Compound: OTX-015; 2	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay	[PMID: 31490070]
MOLM-14	EC₅₀	0.08 μM Compound: OTX015	Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
MV4-11	IC₅₀	0.2 μM Compound: OTX015	Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 33077265]
MV4-11	IC₅₀	17.6 nM Compound: 2; OTX015	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay	[PMID: 31461688]
MV4-11	IC₅₀	46.3 nM Compound: 4; OTX-015	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
NCI-H522	GI₅₀	262.4 nM Compound: OTX-015	Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
ONS-76	GI₅₀	160 nM Compound: OTX-015; MK-8628	Antitumor activity against human ONS-76 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antitumor activity against human ONS-76 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 33636537]
REH	IC₅₀	15.32 μM Compound: OTX-015	Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
RS4-11	IC₅₀	416 nM Compound: 4; OTX-015	Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
SNB-75	GI₅₀	29.6 nM Compound: OTX-015	Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
TALL-1	IC₅₀	1.35 μM Compound: OTX-015	Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
UACC-62	GI₅₀	161.8 nM Compound: OTX-015	Antiproliferative activity against human UACC-62 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human UACC-62 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34731760]

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].

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

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].

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

Clinical Trial

Molecular Weight

491.99

Formula

C₂₅H₂₂ClN₅O₂S

CAS No.

202590-98-5

Appearance

Solid

Color

Off-white to gray

SMILES

O=C(NC1=CC=C(O)C=C1)C[C@H]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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 49 mg/mL (99.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 3 mg/mL (6.10 mM); Clear solution
Protocol 2

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (20.33 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (257 KB) HNMR (242 KB) LCMS (133 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)

References

[1]. J. Kay Noel, et al. Abstract C244: Development of the BET bromodomain inhibitor OTX015. Mol Cancer Ther November 2013 12; C244.

[2]. Marie-Magdelaine Coudé, et al. BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget. 2015 Jul 10; 6(19): 17698–17712.

[3]. Lu P, et al. The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb. Sci Rep. 2016 Apr 12;6:24100

[4]. Vázquez R, et al. The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with RAD001. Oncotarget. 2017 Jan 31;8(5):7598-7613. [Content Brief]

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	[1]. J. Kay Noel, et al. Abstract C244: Development of the BET bromodomain inhibitor OTX015. Mol Cancer Ther November 2013 12; C244. [2]. Marie-Magdelaine Coudé, et al. BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget. 2015 Jul 10; 6(19): 17698–17712. [3]. Lu P, et al. The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb. Sci Rep. 2016 Apr 12;6:24100 [4]. Vázquez R, et al. The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with RAD001. Oncotarget. 2017 Jan 31;8(5):7598-7613. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0326 mL	10.1628 mL	20.3256 mL	50.8140 mL
	5 mM	0.4065 mL	2.0326 mL	4.0651 mL	10.1628 mL
	10 mM	0.2033 mL	1.0163 mL	2.0326 mL	5.0814 mL
	15 mM	0.1355 mL	0.6775 mL	1.3550 mL	3.3876 mL
	20 mM	0.1016 mL	0.5081 mL	1.0163 mL	2.5407 mL
	25 mM	0.0813 mL	0.4065 mL	0.8130 mL	2.0326 mL
	30 mM	0.0678 mL	0.3388 mL	0.6775 mL	1.6938 mL
	40 mM	0.0508 mL	0.2541 mL	0.5081 mL	1.2704 mL
	50 mM	0.0407 mL	0.2033 mL	0.4065 mL	1.0163 mL
	60 mM	0.0339 mL	0.1694 mL	0.3388 mL	0.8469 mL
	80 mM	0.0254 mL	0.1270 mL	0.2541 mL	0.6352 mL

Birabresib Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Birabresib202590-98-5OTX-015 MK-8628OTX015OTX 015MK8628MK 8628MK-8628Epigenetic Reader DomainInhibitorinhibitorinhibit

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

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29 Publications Citing Use of MCE Birabresib

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•Related Screening Libraries:

•Related Small Molecules:

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Birabresib Related Antibodies

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Complete Stock Solution Preparation Table

Birabresib Related Classifications

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