Chemical Properties | Back Directory | [Boiling point ]
512.0±50.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 300 mg/mL (933.36 mM) | [form ]
Solid | [pka]
14.82±0.60(Predicted) | [color ]
White to light yellow |
Hazard Information | Back Directory | [Description]
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor. BRD0705 can be used for acute myeloid leukemia. | [Uses]
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) research[1]. | [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.
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| [IC 50]
GSK3α: 66 nM (IC50); GSK3α: 4.8 μM (Kd); GSK-3β(WT): 515 nM (IC50) | [storage]
Store at -20°C | [References]
[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. DOI:10.1126/scitranslmed.aam8460 |
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Company Name: |
BOC Sciences
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Tel: |
1-631-485-4226; 16314854226 |
Website: |
https://www.bocsci.com |
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