Cat. No.: HY-116830

BRD0705

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BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC₅₀ of 66 nM and a K_d of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC₅₀ of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.

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Pureté: 99.86%
CAS No.: 2056261-41-5
Formule: C₂₀H₂₃N₃O
Masse moléculaire:321.42

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BRD0705 Chemical Structure

CAS No.: 2056261-41-5

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

GSK3α

66 nM (IC₅₀)

GSK3α

4.8 μM (Kd)

GSK-3β(WT)

515 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform GSK-3 :

In Vitro

BRD0705 displays excellent selectivity in a penal of 311 kinases, the CDK family of kinases (CDK2, 3 and 5) are next most potently inhibits at values of 6.87 μM, 9.74 μM and 9.20 μM (87-fold, 123-fold and 116-fold selectivity relative to GSK3α)^[1].
? BRD0705 (10-40 μM; 2-24 hours; U937 cells) treatment impairs GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation^[1].
? Using a β-catenin dependent TCF/LEF luciferase reporter assay, the absence of β-catenin induced target activation after treatment with BRD0705 in AML cell lines^[1].
? BRD0705 impairs AML colony formation in all six tested cell lines, MOLM13, TF-1, U937, MV4-11, HL-60 and NB4, in a concentration-dependent manner, as opposed to BRD3731 which impairs colony formation in TF-1 while increasing colony forming ability in the MV4-11 cell line^[1].

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

Western Blot Analysis^[1]

Cell Line:

U937 cells
Concentration:

10 μM, 20 μM and 40 μM
Incubation Time:

2 hours, 4 hours, 8 hours and 24 hours
Result:

Impaired GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation.

In Vivo

BRD0705 (30 mg/kg; oral gavage; twice daily; NSG mice) treatment impairs leukemia initiation and prolongs survival in AML mouse models^[1].

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

Animal Model:

8-week-old male NSG mice injected with MLL-AF9 AML cells^[1]
Dosage:

30 mg/kg
Administration:

Oral gavage; twice daily
Result:

Mice survival was significantly improved.

Chemical Information

CAS No. 2056261-41-5
Appearance Solid
Masse moléculaire 321.42
Formule C₂₀H₂₃N₃O
Color White to light yellow
SMILES

O=C1C2=C(N=C3C([C@]2(CC)C4=CC=CC=C4)=CNN3)CC(C)(C)C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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SSRN

2023 Jun 20.

Solvant et solubilité

In Vitro:

DMSO : 300 mg/mL (933.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1112 mL

15.5560 mL

31.1119 mL

5 mM

0.6222 mL

3.1112 mL

6.2224 mL

10 mM

0.3111 mL

1.5556 mL

3.1112 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 7.5 mg/mL (23.33 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 7.5 mg/mL (23.33 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 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 (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wagner FF, et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.1112 mL	15.5560 mL	31.1119 mL	77.7798 mL
	5 mM	0.6222 mL	3.1112 mL	6.2224 mL	15.5560 mL
	10 mM	0.3111 mL	1.5556 mL	3.1112 mL	7.7780 mL
	15 mM	0.2074 mL	1.0371 mL	2.0741 mL	5.1853 mL
	20 mM	0.1556 mL	0.7778 mL	1.5556 mL	3.8890 mL
	25 mM	0.1244 mL	0.6222 mL	1.2445 mL	3.1112 mL
	30 mM	0.1037 mL	0.5185 mL	1.0371 mL	2.5927 mL
	40 mM	0.0778 mL	0.3889 mL	0.7778 mL	1.9445 mL
	50 mM	0.0622 mL	0.3111 mL	0.6222 mL	1.5556 mL
	60 mM	0.0519 mL	0.2593 mL	0.5185 mL	1.2963 mL
	80 mM	0.0389 mL	0.1944 mL	0.3889 mL	0.9722 mL
	100 mM	0.0311 mL	0.1556 mL	0.3111 mL	0.7778 mL

Keywords

BRD0705

1 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) BRD0705

Voir tous les produits spécifiques à Isoform GSK-3

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

BRD0705 Related Classifications

HY-116830 Related Classifications