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  3. Epigenetic Reader Domain
  4. Alobresib

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. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.

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

Alobresib Chemical Structure

Alobresib Chemical Structure

CAS No. : 1637771-14-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
1 mg USD 85 In-stock
5 mg USD 180 In-stock
10 mg USD 350 In-stock
25 mg USD 680 In-stock
50 mg USD 1150 In-stock
100 mg USD 1800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Alobresib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Alobresib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research[1][2].

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].

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

Alobresib Related Antibodies

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].

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

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.
Appearance

Solid

Color

Off-white to light yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (190.47 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 2.2858 mL 11.4288 mL 22.8577 mL
5 mM 0.4572 mL 2.2858 mL 4.5715 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2858 mL 11.4288 mL 22.8577 mL 57.1442 mL
5 mM 0.4572 mL 2.2858 mL 4.5715 mL 11.4288 mL
10 mM 0.2286 mL 1.1429 mL 2.2858 mL 5.7144 mL
15 mM 0.1524 mL 0.7619 mL 1.5238 mL 3.8096 mL
20 mM 0.1143 mL 0.5714 mL 1.1429 mL 2.8572 mL
25 mM 0.0914 mL 0.4572 mL 0.9143 mL 2.2858 mL
30 mM 0.0762 mL 0.3810 mL 0.7619 mL 1.9048 mL
40 mM 0.0571 mL 0.2857 mL 0.5714 mL 1.4286 mL
50 mM 0.0457 mL 0.2286 mL 0.4572 mL 1.1429 mL
60 mM 0.0381 mL 0.1905 mL 0.3810 mL 0.9524 mL
80 mM 0.0286 mL 0.1429 mL 0.2857 mL 0.7143 mL
100 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5714 mL
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Alobresib 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:

Alobresib1637771-14-2GS-5829GS5829GS 5829Epigenetic Reader DomainInhibitorinhibitorinhibit

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