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  3. BRD0705

BRD0705 

Cat. No.: HY-116830 Purity: 98.41% ee.: 98.46%
Handling Instructions

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd 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).

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

BRD0705 Chemical Structure

BRD0705 Chemical Structure

CAS No. : 2056261-41-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 715 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1050 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd 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)[1].

IC50 & Target[1]

GSK3α

66 nM (IC50)

GSK3α

4.8 μM (Kd)

GSK-3β(WT)

515 nM (IC50)

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].

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].

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.
Molecular Weight

321.42

Formula

C₂₀H₂₃N₃O

CAS No.

2056261-41-5

SMILES

O=C1C2=C(N=C3C([[email protected]]2(CC)C4=CC=CC=C4)=CNN3)CC(C)(C)C1

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 : 300 mg/mL (933.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

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

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

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

BRD0705BRD 0705BRD-0705GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Acutemyeloidleukemiakinaseoralbioavailabilitysurvivalβ-cateninInhibitorinhibitorinhibit

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BRD0705
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HY-116830
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