Home Epigenetics Epigenetic Reader Domain inhibitor - Apoptosis related activator Mivebresib (ABBV-075) For research use only.

Mivebresib (ABBV-075)

Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.

Mivebresib (ABBV-075) Chemical Structure

Mivebresib (ABBV-075) Chemical Structure

CAS No. 1445993-26-9

Purity & Quality Control

Mivebresib (ABBV-075) Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.0019μM. 32208600
Kasumi-1 Antiproliferative assay 72 hrs Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.0063μM. 32208600
RS4:11 Antiproliferative assay 72 hrs Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.0064μM. 32208600
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.0065μM. 32208600
MX1 Antiproliferative assay 72 hrs Antiproliferative activity against human MX1 cells incubated for 72 hrs by cell-titer Glo assay, EC50=0.013μM. 29678460
MX1 Antiproliferative assay 72 hrs Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay, EC50=0.013μM. 28949521
H1299 Function assay 24 hrs Binding affinity to BRD4 in human H1299 cells stably expressing E2 and HPV16-LCR luciferase reporter incubated for 24 hrs by Bright-Glo luciferase reporter gene assay based BRD4 engagement assay, IC50=0.02μM. 29678460
H1299 Function assay 24 hrs Inhibition of BRD4 in human H1299 cells assessed as decrease in HPV LCR-E2-EP400-mediated transcriptional repression after 24 hrs by Bright-Glo luciferase reporter gene assay, EC50=0.02μM. 28949521
insect cells Function assay Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay, IC50=0.02μM. 30529546
MV411 Antiproliferative assay 72 hrs Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay, IC50=0.07μM. 28314513
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay, IC50=0.09μM. 28314513
HL60 Antiproliferative assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay, IC50=0.12μM. 31857846
SKM1 Antitumor assay 60 mg/kg Antitumor activity against human SKM1 cells xenografted in SCID mouse assessed as tumor growth inhibition at 60 mg/kg, po bid by caliper method 32324999
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Biological Activity

Description Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
Targets
BRD2 [1] BRD4 [1] BRD-T [1]
In vitro
In vitro

ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit[1].
Cell Research Cell lines Macrophages
Concentrations 0.1 µM
Incubation Time 48 h
Method

Cells were treated with indicated concentration of drug for 48 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot BRD4 / c-Myc / CDK6 / Bcl-xL / Bcl-2 / Mcl-1 / HEXIM1 / p21 / p27 / Cleaved PARP 30647404
In Vivo
In vivo

ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04480086 Terminated
Myelofibrosis (MF)
AbbVie
 March 17 2021 Phase 1
NCT02391480 Completed
Cancer|Breast Cancer|Non-Small Cell Lung Cancer|Acute Myeloid Leukemia (AML)|Multiple Myeloma|Prostate Cancer|Small Cell Lung Cancer|Non-Hodgkins Lymphoma
AbbVie
 April 14 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 459.47 Formula

C22H19F2N3O4S
CAS No. 1445993-26-9 SDF Download Mivebresib (ABBV-075) SDF
Smiles CCS(=O)(=O)NC1=CC(=C(C=C1)OC2=C(C=C(C=C2)F)F)C3=CN(C(=O)C4=C3C=CN4)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (198.05 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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