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  3. ABBV-744

ABBV-744 

Cat. No.: HY-112090 Purity: 99.48%
Handling Instructions

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

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

ABBV-744 Chemical Structure

ABBV-744 Chemical Structure

CAS No. : 2138861-99-9

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 770 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values range from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability[1].

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)

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].

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (203.44 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

  • 6.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

  • 7.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution

  • 8.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.48%

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Product Name:
ABBV-744
Cat. No.:
HY-112090
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