Mivebresib
Based on 15 publication(s) in Google Scholar
Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
For research use only. We do not sell to patients.
- Purity: 99.29%
- CAS No.: 1445993-26-9
- Formula: C22H19F2N3O4S
- Molecular Weight:459.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Mivebresib
More- Blood. 2024 Aug 16:blood.2023023644. [Abstract]
- ACS Nano. 2026 May 12;20(18):13624-13635. [Abstract]
- Leukemia. 2025 Dec 19. [Abstract]
- Cell Death Dis. 2019 Jul 19;10(8):557. [Abstract]
- Cell Rep. 2024 Jul 3;43(7):114431. [Abstract]
- J Med Chem. 2020 Jul 9;63(13):7186-7210. [Abstract]
- Eur J Med Chem. 2022 Jun 11;239:114519. [Abstract]
- Biochem Pharmacol. 2021 Mar:185:114435. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- Int Immunopharmacol. 2023 Jul:120:110305. [Abstract]
- Sci Rep. 2024 Apr 20;14(1):9064. [Abstract]
- Anal Sens. 22 June 2022.
- Harvard University. 2026.
- bioRxiv. 2024 Mar 21.
- Martin-Luther-Universität Halle-Wittenberg. 2020 Dec.
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RT-PCR
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WB
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Flow Cytometry
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Cell Proliferation/Viability Assay
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WB
Biological Activity
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BRD4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
1.22 μM
Compound: ABBV-075; 10
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Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36202064] |
| CT26 | IC50 |
48.26 μM
Compound: 6; ABBV-075
|
Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 33862375] |
| GES1 | IC50 |
4.31 nM
Compound: ABBV-075
|
Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 36599264] |
| HCT-116 | IC50 |
0.55 μM
Compound: 8; ABBV-075
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Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 33214826] |
| HepG2 | IC50 |
4.29 nM
Compound: ABBV-075
|
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 36599264] |
| HL-60 | IC50 |
0.09 μM
Compound: ABBV-075
|
Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay
Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay
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[PMID: 28314513] |
| HL-60 | IC50 |
0.12 μM
Compound: 7; Abbv-075
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Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 31857846] |
| HT-29 | IC50 |
1.84 nM
Compound: ABBV-075
|
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 36599264] |
| K562 | IC50 |
>10 μM
Compound: ABBV-075
|
Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay
Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay
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[PMID: 28314513] |
| Kasumi 1 | IC50 |
6.3 nM
Compound: 9; ABBV-075
|
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
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[PMID: 32208600] |
| MCF7 | IC50 |
12.27 nM
Compound: ABBV-075
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 36599264] |
| MM1.S | IC50 |
6.5 nM
Compound: 9; ABBV-075
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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
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[PMID: 32208600] |
| MV4-11 | IC50 |
0.07 μM
Compound: ABBV-075
|
Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay
Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay
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[PMID: 28314513] |
| MV4-11 | IC50 |
1.9 nM
Compound: 9; ABBV-075
|
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
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[PMID: 32208600] |
| MX1 | EC50 |
13 nM
Compound: 5
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Antiproliferative activity against human MX1 cells incubated for 72 hrs by cell-titer Glo assay
Antiproliferative activity against human MX1 cells incubated for 72 hrs by cell-titer Glo assay
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[PMID: 29678460] |
| MX1 | EC50 |
13 nM
Compound: 63; ABBV-075
|
Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay
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[PMID: 28949521] |
| RS4-11 | IC50 |
6.4 nM
Compound: 9; ABBV-075
|
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] |
| U-266 | IC50 |
2.03 μM
Compound: 6; ABBV-075
|
Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
|
[PMID: 33862375] |
Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1445993-26-9
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Appearance Solid
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Molecular Weight 459.47
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Formula C22H19F2N3O4S
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Color White to off-white
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SMILES
CCS(=O)(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)=O
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Synonyms
ABBV-075
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (15)
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Journal Impact Factor
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Most Recent
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Blood
Epigenetic Regulation of Non-canonical Menin Targets Modulates Menin Inhibitor Response in Acute Myeloid Leukemia. [Abstract]2024 Aug 16:blood.2023023644. PMID: 39158067 -
ACS Nano
Nanopore Discrimination of Protein-Small-Molecule Drug Complexes at Near-Atomic Resolution. [Abstract]2026 May 12;20(18):13624-13635. PMID: 42046448 -
Leukemia
BET inhibitor-based combinations targeting novel dependencies in MECOM-rearranged (r) AML. [Abstract]2025 Dec 19. PMID: 41419608
Mivebresib purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Dec 19. [Abstract]
UCSD-AML1 and AML194 cells were treated with 500 nM of mivebresib as biologic replicates for 16 h. Total RNA was isolated and utilized for cDNA generation and qPCR analysis. Messenger RNA expression is normalized to GAPDH and expressed relative to the DMSO control cells. Columns, mean of three replicates; Bars, standard error of the mean (S.E.M.).
Mivebresib purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Dec 19. [Abstract]
AML191, AML194, and UCSD-AML1 cells were treated with the indicated concentrations of Mivebresib (100-1000 nM) for 24 h. At the end of treatment, cells were harvested, total cell lysates were prepared, and immunoblot analyses were conducted. The expression levels of β-Actin in the total cell lysates served as the loading control. Representative blots of at least two experiments are shown.
Mivebresib purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Dec 19. [Abstract]
MUTZ-3, UCSD-AML1, AML191 and AML194 cells were treated with the indicated concentrations of Mivebresib (50-1000 nM) for 48 h. Following this, cells were stained with annexin V-FITC and TO-PRO-3 iodide and the % apoptotic cells were analyzed by flow cytometry.
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Cell Death Dis
Inhibition of the BET family reduces its new target gene IDO1 expression and the production of L-kynurenine. [Abstract]2019 Jul 19;10(8):557. PMID: 31324754
Mivebresib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 19;10(8):557. [Abstract]
BET inhibitors reduce IDO1 transcription.The protein levels of IDO1 are determined by RT-qPCR and western blotting, respectively.
Mivebresib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 19;10(8):557. [Abstract]
ABBV-075 (Mivebresib, 10-100 nM; 3-24 h) reduces the mRNA levels of IDO1 in concentration- and time-dependent manners in Ty-82 cells.
Mivebresib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 19;10(8):557. [Abstract]
ABBV-075 (Mivebresib, 10-100 nM; 3-24 h) reduces the protein levels of IDO1 in concentration- and time-dependent manners in Ty-82 cells.
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Cell Rep
Elevating PLK1 overcomes BETi resistance in prostate cancer via triggering BRD4 phosphorylation-dependent degradation in mitosis. [Abstract]2024 Jul 3;43(7):114431. PMID: 38968071
Mivebresib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Jul 3;43(7):114431. [Abstract]
The cell viability of C4-2/tet-PLK1 cells upon dosages of ABBV-075 (Mivebresib) treatment. ** P < 0.01.
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J Med Chem
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. [Abstract]2020 Jul 9;63(13):7186-7210. PMID: 32453591 -
Eur J Med Chem
Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities. [Abstract]2022 Jun 11;239:114519. PMID: 35714446
Mivebresib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2022 Jun 11;239:114519. [Abstract]
Protein levels of IDO1 and c-Myc. Ty-82 cells were treated with ABBV-075 (Mivebresib, 0.1-10 nM), or 21 for 24 h and collected for Western blotting.
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Biochem Pharmacol
Novel bivalent BET inhibitor N2817 exhibits potent anticancer activity and inhibits TAF1. [Abstract]2021 Mar:185:114435. PMID: 33539817
Mivebresib purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Mar:185:114435. [Abstract]
Protein levels of IDO1 and c-Myc. Ty-82 cells were treated with 8124-053, ABBV-075 (Mivebresib, 0.1-10 nM), or N2817 for 24 h and collected for western blotting.
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Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
Int Immunopharmacol
Mivebresib alleviates systemic lupus erythematosus-associated diffuse alveolar hemorrhage via inhibiting infiltration of monocytes and M1 polarization of macrophages. [Abstract]2023 Jul:120:110305. PMID: 37182455 -
Sci Rep
Epigenetic modulation through BET bromodomain inhibitors as a novel therapeutic strategy for progranulin-deficient frontotemporal dementia. [Abstract]2024 Apr 20;14(1):9064. PMID: 38643236 -
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Solvent & Solubility
DMSO : 100 mg/mL (217.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.44 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.44 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 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1764 mL | 10.8821 mL | 21.7642 mL | 54.4105 mL |
| 5 mM | 0.4353 mL | 2.1764 mL | 4.3528 mL | 10.8821 mL | |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1764 mL | 5.4411 mL | |
| 15 mM | 0.1451 mL | 0.7255 mL | 1.4509 mL | 3.6274 mL | |
| 20 mM | 0.1088 mL | 0.5441 mL | 1.0882 mL | 2.7205 mL | |
| 25 mM | 0.0871 mL | 0.4353 mL | 0.8706 mL | 2.1764 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7255 mL | 1.8137 mL | |
| 40 mM | 0.0544 mL | 0.2721 mL | 0.5441 mL | 1.3603 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
| 60 mM | 0.0363 mL | 0.1814 mL | 0.3627 mL | 0.9068 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2721 mL | 0.6801 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 mL |