BRD0705

Catalog No.S9638 Batch:S963801

Technical Data

Formula

C₂₀H₂₃N₃O

Molecular Weight

321.42

CAS No.

2056261-41-5

Solubility (25°C)*

In vitro

DMSO

64 mg/mL (199.11 mM)

Ethanol

64 mg/mL (199.11 mM)

Water

Insoluble

In Vivo (Add solvents to the product individually and in order.)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (10.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.530mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. This compound also inhibits GSK3β with IC50 of 515 nM. It can be used for acute myeloid leukaemia (AML).

Targets

GSK3α (Cell-free assay)	GSK3β (Cell-free assay)	GSK3α (Cell-free assay)
66 nM	515 nM(Kd)	4.8 μM(Kd)

In vitro

BRD0705 inhibits kinase function and does not stabilise β-catenin, mitigating potential neoplastic concerns. This compound induces myeloid differentiation and impairs colony formation in AML cells while no effect is observed on normal haematopoietic cells.

In Vivo

This compound impairs leukaemia initiation and prolongs survival in AML mouse models.

Protocol (from reference)

Cell Assay:^{^[1]}	Cell Lines HEK 293T, HL-60, U937, TF-1, NB-4, MV4–11, MOLM-13, Mononuclear cells Concentrations 20 μM Incubation Time 24 hours Method After 24 hours of treatment with DMSO or BRD0705 at 20 μM, 30,000 to 50,000 cells are washed in PBS/2%FBS and then cytospun onto poly-L-Lysine coated slides (EMS). Cells are fixed in 4% paraformaldehyde (EMS) for 20 minutes, permeabilized in 0.2% Triton X-100 (RPI) for 30 minutes at 4°C, blocked in 1% BSA/0.05% triton for 1 hour at room temperature and then incubated for 1 hour at room temperature with primary anti-β-catenin (1/500) and then secondary antibody. Three 5 minute washes are performed after each antibody incubation. Slides are mounted with Prolong (R) Gold Antifade with DAPI and imaged with Yokogawa Spinning Disk Confocal / TIRF system. Representative images of three independent experiments are analyzed with Image-J software.
Animal Study:^{^[1]}	Animal Models 8-week-old male NSG mice Dosages 15 mg/kg, 30 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

Cell Lines
HEK 293T, HL-60, U937, TF-1, NB-4, MV4–11, MOLM-13, Mononuclear cells
Concentrations
20 μM
Incubation Time
24 hours
Method
After 24 hours of treatment with DMSO or BRD0705 at 20 μM, 30,000 to 50,000 cells are washed in PBS/2%FBS and then cytospun onto poly-L-Lysine coated slides (EMS). Cells are fixed in 4% paraformaldehyde (EMS) for 20 minutes, permeabilized in 0.2% Triton X-100 (RPI) for 30 minutes at 4°C, blocked in 1% BSA/0.05% triton for 1 hour at room temperature and then incubated for 1 hour at room temperature with primary anti-β-catenin (1/500) and then secondary antibody. Three 5 minute washes are performed after each antibody incubation. Slides are mounted with Prolong (R) Gold Antifade with DAPI and imaged with Yokogawa Spinning Disk Confocal / TIRF system. Representative images of three independent experiments are analyzed with Image-J software.

Animal Study:^{^[1]}

Animal Models
8-week-old male NSG mice
Dosages
15 mg/kg, 30 mg/kg
Administration
Oral gavage

References

https://pubmed.ncbi.nlm.nih.gov/29515000/

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.