ABBV-744

Name: ABBV-744
Brand: MedChemExpress
SKU: HY-112090
Rating: 5.0 (11 reviews)

Cat. No.: HY-112090 Purity: 99.97%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC₅₀ values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.

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

CAS No. : 2138861-99-9

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
1 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 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE ABBV-744

Bio/Physico-chemical Assay

ELISA

RT-PCR

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM) for 2 h and then exposed to LPS (100 ng/mL) for 24 h (n = 5). The production of NO was measured using nitric oxide detection kit.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM) for 2 h and then exposed to LPS (100 ng/mL) for 24 h (n = 5). The levels of pro-inflammatory factors TNF-α and IL-6 were measured using ELISA.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.01, 0.03, 0.1 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 5). The mRNA levels of TNF-α, IL-1β and IL-6 were measured by quantitative real-time PCR.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.01, 0.03, 0.1 μM) for 2 h and then exposed to LPS (100 ng/mL) for 24 h (n = 5). The protein levels of iNOS, COX2 and α-tubulin were measured using immunoblot analysis.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; Primary microglial cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 5). The mRNA levels of TNF-α, IL-1β, and IL-6 were measured by quantitative real-time PCR.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; C57BL/6J mice were treated with vehicle (5% DMSO + 40% PEG300 + 55% saline; p.o.) or ABBV-744 (0.05, 0.1, 0.2 mg/kg; p.o.) daily for 2 days, followed by injection with saline or LPS (5 mg/kg; i.p.) for 1 day. Activation of microglia in the CA1 region of mice hippocampus was detected by immunofluorescence staining using an anti-Iba1 antibody.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; C57BL/6J mice were treated with vehicle (5% DMSO + 40% PEG300 + 55% saline; p.o.) or ABBV-744 (0.05, 0.1, 0.2 mg/kg; p.o.) daily for 2 days, followed by injection with saline or LPS (5 mg/kg; i.p.) for 1 day. The mRNA levels of TNF-α and IL-1β in the hippocampus were measured by quantitative real-time PCR (n = 7–8).

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 4–5). The mRNA levels of BATF2 and IRF4 were measured by quantitative real-time PCR.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 15 min (n = 5). The protein level of BATF2 was measured by Western blot. The quantification of the intensity of BATF2 relative to β-actin is shown.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 6–7). Protein levels of p-JAK2 and JAK2, p-STAT1 and STAT1 were measured by Western blot and β-actin or GAPDH were used as a loading control.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 6–7). Protein levels of p-STAT3 and STAT3, p-STAT5 and STAT5 were measured by Western blot and β-actin or GAPDH were used as a loading control.

: ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]; C57BL/6J mice were treated with vehicle (5% DMSO + 40% PEG300 + 55% saline; p.o.) or ABBV-744 (0.1 mg/kg; p.o.) daily for 2 days, followed by injection with saline or LPS (5 mg/kg; i.p.) for 1 day. Protein levels of BATF2 and IRF4 were measured by Western blot and β-actin was used as a loading control.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

BRD2 (BD2)

8 nM (IC₅₀)

BRD3 (BD2)

13 nM (IC₅₀)

BRDT (BD2)

18 nM (IC₅₀)

BRD4 (BD2)

4 nM (IC₅₀)

BRD4 (BD2)

3 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	20700 nM Compound: 46; ABBV-744	Inhibition of NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay Inhibition of NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay	[PMID: 32324999]
HeLa	IC₅₀	27.5 nM Compound: 46; ABBV-744	Inhibition of NanoLuc-tagged BRD4 BD2 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay Inhibition of NanoLuc-tagged BRD4 BD2 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay	[PMID: 32324999]
MOLM-13	IC₅₀	0.039 μM Compound: 10; ABBV-744	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay	[PMID: 38175809]
MV4-11	IC₅₀	0.015 μM Compound: 10; ABBV-744	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay	[PMID: 38175809]
MV4-11	IC₅₀	0.04 μM Compound: ABBV-744	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell growth Antiproliferative activity against human MV4-11 cells assessed as reduction in cell growth	[PMID: 38964169]
MV4-11	IC₅₀	0.25 μM Compound: ABBV-744	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	152.67 nM Compound: ABBV-744	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay	[PMID: 35395439]
NCI-H1299	IC₅₀	1600 nM Compound: 46; ABBV-744	Antiproliferative activity against human H1299 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Antiproliferative activity against human H1299 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 32324999]
SKM-1	IC₅₀	6.7 nM Compound: 46; ABBV-744	Antiproliferative activity against human SKM1 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Antiproliferative activity against human SKM1 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 32324999]

In Vitro

ABBV-744 (90 nM; 0~24 h; LNCaP cells) downregulates the expression of KLK2 and MYC genes^[1].
? ABBV-744 (90 nM; 0~72 h; LNCaP cells) induces cell cycle arrest in G1 followed by senescence^[1].

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

Western Blot Analysis^[1]

Cell Line:	LNCaP cells
Concentration:	90 nM
Incubation Time:	0~24 hours
Result:	Downregulated the expression of KLK2 and MYC genes.

Cell Cycle Analysis^[1]

Cell Line:	LNCaP cells
Concentration:	90 nM
Incubation Time:	0~72 hours
Result:	Induced cell cycle arrest in G1 followed by senescence.

In Vivo

ABBV-744 (4.7 mg/kg; oral gavage; 28 days) causes a delay in tumor growth and displays equivalent or better antitumor activity compared with ABBV-075^[1].
? ABBV-744 (30 mg/kg; 14 days) is able to produce significant antitumor activity. ABBV-744 (30 mg/kg) triggers a reduction in platelets of only 20 %^[1].

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

Animal Model:	Mice
Dosage:	4.7 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral gavage; 28 days
Result:	Caused a delay in tumor growth and displayed equivalent or better antitumor activity compared with ABBV-075.

Animal Model:	Sprague-Dawley rats
Dosage:	30 mg/kg (Pharmacokinetic Analysis)
Administration:	14 days
Result:	Produced significant antitumor activity.

Clinical Trial

Molecular Weight

491.55

Formula

C₂₈H₃₀FN₃O₄

CAS No.

2138861-99-9

Appearance

Solid

Color

White to light yellow

SMILES

CC(O)(C)C1=CC(C(C2=C3NC(C(NCC)=O)=C2)=CN(C)C3=O)=C(OC4=C(C)C=C(F)C=C4C)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (203.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0344 mL	10.1719 mL	20.3438 mL
5 mM	0.4069 mL	2.0344 mL	4.0688 mL
10 mM	0.2034 mL	1.0172 mL	2.0344 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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 (5.09 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 (5.09 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 (5.09 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.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (4.07 mM); Clear 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: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

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).

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

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: 99.97%

Select Batch:

Data Sheet (285 KB) SDS (394 KB)

COA (259 KB) HNMR (190 KB) RP-HPLC (254 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Faivre EJ, et al. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer. Nature. 2020;578(7794):306-310. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0344 mL	10.1719 mL	20.3438 mL	50.8595 mL
	5 mM	0.4069 mL	2.0344 mL	4.0688 mL	10.1719 mL
	10 mM	0.2034 mL	1.0172 mL	2.0344 mL	5.0860 mL
	15 mM	0.1356 mL	0.6781 mL	1.3563 mL	3.3906 mL
	20 mM	0.1017 mL	0.5086 mL	1.0172 mL	2.5430 mL
	25 mM	0.0814 mL	0.4069 mL	0.8138 mL	2.0344 mL
	30 mM	0.0678 mL	0.3391 mL	0.6781 mL	1.6953 mL
	40 mM	0.0509 mL	0.2543 mL	0.5086 mL	1.2715 mL
	50 mM	0.0407 mL	0.2034 mL	0.4069 mL	1.0172 mL
	60 mM	0.0339 mL	0.1695 mL	0.3391 mL	0.8477 mL
	80 mM	0.0254 mL	0.1271 mL	0.2543 mL	0.6357 mL
	100 mM	0.0203 mL	0.1017 mL	0.2034 mL	0.5086 mL

ABBV-744 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:

ABBV-7442138861-99-9ABBV744ABBV 744Epigenetic Reader DomainHIVHuman immunodeficiency virusLNCaPAntitumorPotentOralSelectiveDrug-likeCYP3A4Inhibitorinhibitorinhibit

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ABBV-744

Customer Review

ABBV-744 Related Antibodies

11 Publications Citing Use of MCE ABBV-744

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Biological Activity

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Customer Review

ABBV-744 Related Antibodies

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Complete Stock Solution Preparation Table

ABBV-744 Related Classifications

Keywords:

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