| Identification | Back Directory | [Name]
(Rac)-BRD0705 | [CAS]
1597440-03-3 | [Synonyms]
(Rac)-BRD0705
5H-Pyrazolo[3,4-b]quinolin-5-one, 4-ethyl-1,2,4,6,7,8-hexahydro-7,7-dimethyl-4-phenyl-
GSK3α,inhibit,Racemate,(Rac)BRD0705,GSK-3,Inhibitor,Glycogen synthase kinase-3,(Rac) BRD0705,(Rac)-BRD-0705,Glycogen synthase kinase 3,(Rac)-BRD0705 | [Molecular Formula]
C20H23N3O | [MOL File]
1597440-03-3.mol | [Molecular Weight]
321.42 |
| Chemical Properties | Back Directory | [Boiling point ]
512.0±50.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
14.82±0.60(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
(Rac)-BRD0705 is a less active racemate of BRD0705. 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][2]. | [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
[2] Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1. |
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