1. Epigenetics
  2. Epigenetic Reader Domain
  3. Alobresib

Alobresib (Synonyms: GS-5829)

Cat. No.: HY-109050 Purity: 98.07%
Handling Instructions

Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc.

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

Alobresib Chemical Structure

Alobresib Chemical Structure

CAS No. : 1637771-14-2

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10 mM * 1  mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
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10 mg USD 350 In-stock
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25 mg USD 680 In-stock
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50 mg USD 1150 In-stock
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100 mg USD 1800 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc[1].

IC50 & Target

BET bromodomain[1]

In Vitro

Alobresib (0.1 nM-100 μM; 72 hours) inhibits cell proliferation in primary uterine serous carcinoma (USC) lines[1].

Cell Proliferation Assay[1]

Cell Line: Primary uterine serous carcinoma (USC) lines ARK1 and ARK2 cell lines
Concentration: 0.1 nM, 10 nM, 1 μM, 100 μM
Incubation Time: 72 hours
Result: A progressive, dose response decrease in cell proliferation. IC50s of 27 nM and 31 nM for ARK2 and ARK1 cells, respectively.
In Vivo

Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) impaires USC-ARK2 xenograft tumor growth in female CB17/lcrHsd-Prkd/scid mice. Alobresib exhibits a significantly slower rate of tumor growth in mice, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.)[1].
Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) is well tolerated with no clear impact on body weight compared with vehicle control[1].

Animal Model: Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors[1]
Dosage: 10 and 20 mg/kg
Administration: Oral; twice-daily; 28 days
Result: Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).
Clinical Trial
Molecular Weight

437.49

Formula

C₂₆H₂₃N₅O₂

CAS No.

1637771-14-2

SMILES

OC(C1=CC=CC=N1)(C2=CC=CC=N2)C3=C(NC(C4CC4)=N5)C5=CC(C(C(C)=NO6)=C6C)=C3

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 : 83.33 mg/mL (190.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2858 mL 11.4288 mL 22.8577 mL
5 mM 0.4572 mL 2.2858 mL 4.5715 mL
10 mM 0.2286 mL 1.1429 mL 2.2858 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: ≥ 2.08 mg/mL (4.75 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

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

AlobresibGS-5829GS5829GS 5829Epigenetic Reader DomainInhibitorinhibitorinhibit

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Alobresib
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