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Mivebresib (ABBV-075)

Name: Mivebresib (ABBV-075)
Brand: Selleck Chemicals
SKU: S8400
Rating: 5 (14 reviews)

Catalog No.S8400 Purity:99.97%

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

CAS No. 1445993-26-9

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Mivebresib (ABBV-075) Related Products

Related Targets	BET p300/CBP BRPF bromodomain	Click to Expand
Related Products	ICG-001 Birabresib (OTX015) I-BET151 (GSK1210151A) Molibresib (I-BET-762) SGC-CBP30 EED226 Apabetalone (RVX-208) KG-501 CPI-203 compound 3i (666-15) PFI-3 AZD5153 6-hydroxy-2-naphthoic acid PFI-1 (PF-6405761) ABBV-744 UNC1215 I-BRD9 Bromosporine PLX51107 GSK1324726A (I-BET726) Pelabresib (CPI-0610) PF-CBP1 HCl INCB054329 MS436 GSK2801 UNC669 MZ-1 NEO2734 OF-1 CPI-637 GSK6853 I-CBP112 BI-7273 PFI-4 INCB057643 GSK 5959 dBET57 BI-9564 Histone Acetyltransferase Inhibitor II	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	Click to Expand

Signaling Pathway

Epigenetic Reader Domain Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Biological Activity

Description

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
Experimental Result Images	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (5.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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