製品番号: HY-15743

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Birabresib

(別名: OTX-015; MK-8628)

41 Cited Publications

カスタマーレビュー

Based on 41 publication(s) in Google Scholar

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

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純度: 99.96%
CAS 番号: 202590-98-5
分子式: C₂₅H₂₂ClN₅O₂S
分子量:491.99

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Birabresib 構造式

CAS 番号: 202590-98-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (41)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
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生物活性

製品説明

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]

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
BJAB	GI₅₀	0.13 μM Compound: 11; OTX-015	Antiproliferative activity against human BJAB cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human BJAB cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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]
D283 Med	IC₅₀	0.066 μM Compound: 1c	Antiproliferative activity against human D283 Med cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human D283 Med cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 36898329]
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]
Daudi	GI₅₀	4 μM Compound: 11; OTX-015	Antiproliferative activity against human Daudi cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human Daudi cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human K562 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human K562 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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]
KU-19-19	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human KU-19-19 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human KU-19-19 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
Leukemia cell	IC₅₀	92 nM Compound: OTX-015	Antiproliferative activity against human Acute myeloid leukemic cells Antiproliferative activity against human Acute myeloid leukemic cells	[PMID: 38749341]
LNCaP	IC₅₀	111.4 nM Compound: 3; OTX-015	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 29758518]
LS-1034	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human LS1034 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human LS1034 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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-13	IC₅₀	0.011 μM Compound: 1c	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 36898329]
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]
MOLT-4	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human MOLT-4 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human MOLT-4 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
MV4-11	GI₅₀	0.03 μM Compound: 11; OTX-015	Cytotoxicity against human MV4-11 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Cytotoxicity against human MV4-11 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
MV4-11	IC₅₀	0.022 μM Compound: 1c	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 36898329]
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-H1666	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human NCI-H1666 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human NCI-H1666 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
NCI-H1975	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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]
Pfeiffer	GI₅₀	0.21 μM Compound: 11; OTX-015	Antiproliferative activity against human Pfeiffer cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human Pfeiffer cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
Raji	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human Raji cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human Raji cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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]
SUD4	GI₅₀	2.8 μM Compound: 11; OTX-015	Antiproliferative activity against human SU-DHL-4 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human SU-DHL-4 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
T-24	GI₅₀	7.9 μM Compound: 11; OTX-015	Antiproliferative activity against human T24 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human T24 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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]
THP-1	GI₅₀	0.04 μM Compound: 11; OTX-015	Antiproliferative activity against human THP-1 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human THP-1 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
THP-1	IC₅₀	0.033 μM Compound: IV; OTX-015; MK8658	Antiproliferative activity against human THP1 cells Antiproliferative activity against human THP1 cells	[PMID: 28939121]
U2932	GI₅₀	>10 μM Compound: 11; OTX-015	Antiproliferative activity against human U2932 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay Antiproliferative activity against human U2932 cells assessed as growth inhibition incubated for 72 hrs by WST-1 assay	[PMID: 38134745]
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]

体外実験

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.

体内実験

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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 202590-98-5
性状 Solid
分子量 491.99
分子式 C₂₅H₂₂ClN₅O₂S
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
別名

OTX-015; MK-8628
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (41)

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Cell

Targeting Epigenetic Crosstalk as a Therapeutic Strategy for EZH2-Aberrant Solid Tumors. [Abstract]

2018 Sep 20;175(1):186-199.e19. PMID: 30220457
Blood

Overcoming menin inhibitor resistance in AML cells with combinations including BET proteins and a dual BRG1/BRM inhibitor. [Abstract]

2026 Feb 24:blood.2025031486. PMID: 41734382
Cancer Res

SWI/SNF-Compromised Cancers Are Susceptible to Bromodomain Inhibitors. [Abstract]

2019 May 15;79(10):2761-2774. PMID: 30877105

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.
Cancer Res

Tailoring Chemotherapy for the African-Centric S47 Variant of TP53. [Abstract]

2018 Oct 1;78(19):5694-5705. PMID: 30115697
Hepatology

Aberrant Super-Enhancer Landscape in Human Hepatocellular Carcinoma. [Abstract]

2019 Jun;69(6):2502-2517. PMID: 30723918
Nat Commun

BET inhibitors drive Natural Killer activation in non-small cell lung cancer via BRD4 and SMAD3. [Abstract]

2024 Mar 22;15(1):2567. PMID: 38519469
Hemasphere

Highly effective combination of BRG1/BRM inhibitor with BET inhibitor or decitabine for high-risk MECOM-rearranged AML. [Abstract]

2026 Jan 15;10(1):e70289. PMID: 41551728
J Exp Clin Cancer Res

KLF7 regulates super-enhancer-driven IGF2BP2 overexpression to promote the progression of head and neck squamous cell carcinoma. [Abstract]

2024 Mar 5;43(1):69. PMID: 38443991
J Exp Clin Cancer Res

A novel dual epigenetic approach targeting BET proteins and HDACs in Group 3 (MYC-driven) Medulloblastoma. [Abstract]

2022 Nov 11;41(1):321. PMID: 36357906
J Exp Med

Bromodomain protein BRD4 directs and sustains CD8 T cell differentiation during infection. [Abstract]

2021 Aug 2;218(8):e20202512. PMID: 34037670
Proc Natl Acad Sci U S A

CDK7 inhibition suppresses aberrant hedgehog pathway and overcomes resistance to smoothened antagonists. [Abstract]

2019 Jun 25;116(26):12986-12995. PMID: 31182587
Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
EMBO Mol Med

Co-targeting BET and MEK as salvage therapy for MAPK and checkpoint inhibitor-resistant melanoma. [Abstract]

2018 May;10(5). pii: e8446. PMID: 29650805

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.
J Transl Med

The BRD4 inhibitor JQ1 suppresses tumor growth by reducing c-Myc expression in endometrial cancer. [Abstract]

2022 Jul 28;20(1):336. PMID: 35902869
Oncogene

Synergistic effects of combined BET and FAK inhibition against Vestibular Schwannomas in NF2-related Schwannomatosis. [Abstract]

2024 Sep;43(40):2995-3002. PMID: 39209965
Oncogene

Therapeutic targeting the oncogenic driver EWSR1::FLI1 in Ewing sarcoma through inhibition of the FACT complex. [Abstract]

2023 Jan;42(1):11-25. PMID: 36357572
Blood Adv

Preclinical efficacy of tasquinimod-based combinations in advanced myeloproliferative neoplasms (MPN) in blastic phase. [Abstract]

2025 Aug 19:bloodadvances.2025016898. PMID: 40829105
Chin Med

Cayratia albifolia C.L.Li exerts anti-rheumatoid arthritis effect by inhibiting macrophage activation and neutrophil extracellular traps (NETs). [Abstract]

2024 Mar 5;19(1):42. PMID: 38444022
Biochem Pharmacol

Co-inhibition of BET and NAE enhances BIM-dependent apoptosis with augmented cancer therapeutic efficacy. [Abstract]

2024 May:223:116198. PMID: 38588830
Mol Cancer Ther

Reprogramming of Nucleotide Metabolism Mediates Synergy between Epigenetic Therapy and MAP Kinase Inhibition. [Abstract]

2021 Jan;20(1):64-75. PMID: 33087508
PLoS Pathog

BRD4 inhibition exerts anti-viral activity through DNA damage-dependent innate immune responses. [Abstract]

2020 Mar 24;16(3):e1008429. PMID: 32208449
Cancers (Basel)

Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]

2024 Aug 7;16(16):2785. PMID: 39199558
Cancers

Systems Biology Approach Identifies Prognostic Signatures of Poor Overall Survival and Guides the Prioritization of Novel BET-CHK1 Combination Therapy for Osteosarcoma. [Abstract]

2020 Aug 26;12(9):2426. PMID: 32859084
iScience

AURKA and PLK1 inhibition selectively and synergistically block cell cycle progression in diffuse midline glioma. [Abstract]

2022 May 13;25(6):104398. PMID: 35637734
J Biol Chem

Low-dose EGFR inhibition unlocks ferroptosis susceptibility to sensitize chemotherapy in EGFR-high triple-negative breast cancer. [Abstract]

2026 May 25:113185. PMID: 42190815
Cancer Med

Development of a novel cell line-derived xenograft model of primary herpesvirus 8-unrelated effusion large B-cell lymphoma and antitumor activity of birabresib in vitro and in vivo. [Abstract]

2021 Dec;10(24):8976-8987. PMID: 34821060
Noncoding RNA

Bromodomain and Extra-Terminal Family Proteins BRD2, BRD3, and BRD4 Contribute to H19-Dependent Transcriptional Regulation of Cell Adhesion Molecules, Modulating Metastatic Dissemination Program in Prostate Cancer. [Abstract]

2025 Apr 29;11(3):33. PMID: 40407591
Am J Cancer Res

TNKS inhibitors potentiate proliferative inhibition of BET inhibitors via reducing β-Catenin in colorectal cancer cells. [Abstract]

2022 Mar 15;12(3):1069-1087. PMID: 35411247
Biochem Biophys Res Commun

The CDK4/6-UCHL5-BRD4 axis confers resistance to BET inhibitors in MLL-rearranged leukemia cells by suppressing BRD4 protein degradation. [Abstract]

2022 Jan 15:588:147-153. PMID: 34954522
Leuk Res Rep

2025 Dec 20.
Harvard University

2026.
bioRxiv

Divergent condensates tune transcriptional responses during stress. [Abstract]

2026 Feb 13:2026.02.12.705659. PMID: 41727155
bioRxiv

Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]

2026 Feb 18:2026.02.16.706212. PMID: 41757027
bioRxiv

2026 Jan 9.
bioRxiv

BRD2 Upregulation as a Pan-Cancer Adaptive Resistance Mechanism to BET Inhibition. [Abstract]

2025 Sep 3:2025.08.30.673282. PMID: 40949948
bioRxiv

2023 Oct 1.
University of Gothenburg

2023 Jun 27.
Technische Universität München

2022.
Research Square Preprint

2021 Jun.
Patent

US20180263995A1.
Oncotarget

Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma-an aggressive and fatal disease. [Abstract]

2017 Dec 2;8(68):112313-112329. PMID: 29348827

溶剤 & 溶解度

体外:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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.

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

プロトコル

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.

MedChemExpress (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.

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (285 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Birabresib

41 Cited Publications

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Birabresib

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

MedChemExpress（MCE）の使用を引用している文献 Birabresib

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (41)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Birabresib

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

MedChemExpress（MCE）の使用を引用している文献 Birabresib

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (41)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Birabresib 関連分類

HY-15743 関連分類