AZD2858 AZD 2858; AZD-2858 CAS 486424-20-8
AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway.

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AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway.
IC50 Value: 68 nM [1]
Target: GSK3
in vitro: Treatment (1 ¦ÌM) of human osteoblast cells with AZD2858 in vitro increased ¦Â-catenin levels after a short period of time. AZD2858 treatment (1 ¦ÌM, 12 h) on primary isolated human osteoblast-like cells results in a 3-fold increase of ¦Â-catenin levels [1].
in vivo: In rats, oral AZD2858 treatment caused a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect at a dose of 20 mg/kg once daily (total BMC: 172% of control; p<0.001). A small but significant effect was also seen at cortical sites (total BMC: 111% of control; p<0.001). Biomechanical testing demonstrated an increase in both vertebral compression strength at a dose of 20 mg/kg once daily (Load at failure: 370% of control, p<0.001) and diaphyseal strength of femora subjected to a three point bending test (Load at failure: 115% of control; p<0.01) [1]. The rats were treated with oral administration of AZD2858 at a dose of 30 ¦Ìmol/kg (20mg/kg) daily for up to 3 weeks, while control animals were administered vehicle. At 4days, and at 1, 2 and 3 weeks, histological analysis was performed, and at the 2 and 3 week time points, we performed peripheral quantitative computed tomography (pQCT), X-rays, and four-point bending tests [2].
Toxicity:
Clinical triaL

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