Mivebresib (Synonyms: ABBV-075)

Name: Mivebresib
Brand: MedChemExpress
SKU: HY-100015
Rating: 5.0 (12 reviews)

Cat. No.: HY-100015 Purity: 99.29%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K_i of 1.5 nM.

For research use only. We do not sell to patients.

Mivebresib Chemical Structure

CAS No. : 1445993-26-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Mivebresib:

Mivebresib (Standard) Get quote

11 Publications Citing Use of MCE Mivebresib

: 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.

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Biological Activity
Purity & Documentation
References
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Description

Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K_i of 1.5 nM^[1].

IC₅₀ & Target

IC50: 1.5 nM (BRD4)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	1.22 μM Compound: ABBV-075; 10	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	[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	[PMID: 36599264]
HCT-116	IC₅₀	0.55 μM Compound: 8; ABBV-075	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	[PMID: 28314513]
HL-60	IC₅₀	0.12 μM Compound: 7; Abbv-075	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	[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	[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	[PMID: 36599264]
MM1.S	IC₅₀	6.5 nM Compound: 9; ABBV-075	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]
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	[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	[PMID: 32208600]
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	[PMID: 28949521]
MX1	EC₅₀	13 nM Compound: 5	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	[PMID: 29678460]
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]

In Vitro

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.

Clinical Trial

Molecular Weight

459.47

Formula

C₂₂H₁₉F₂N₃O₄S

CAS No.

1445993-26-9

Appearance

Solid

Color

White to off-white

SMILES

CCS(=O)(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1764 mL	10.8821 mL	21.7642 mL
5 mM	0.4353 mL	2.1764 mL	4.3528 mL
10 mM	0.2176 mL	1.0882 mL	2.1764 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, 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.

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: 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.44 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.

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: 99.29%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (253 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. EJ Faivre et al. Abstract 4694: ABBV-075, a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo

Complete Stock Solution Preparation Table

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

Mivebresib Related Classifications

Help & FAQs

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:

Mivebresib1445993-26-9ABBV-075ABBV075ABBV 075Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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Mivebresib (Synonyms: ABBV-075)

Customer Review

Other Forms of Mivebresib:

Mivebresib Related Antibodies

11 Publications Citing Use of MCE Mivebresib

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Biological Activity

Purity & Documentation

References

Customer Review

Mivebresib Related Antibodies

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Complete Stock Solution Preparation Table

Mivebresib Related Classifications

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