Molecular Formula | C28H25FN6O3 |
Molar Mass | 512.53 |
Density | 1.55±0.1 g/cm3(Predicted) |
Solubility | Soluble in DMSO, not in water |
Appearance | powder |
Color | yellow to orange |
pKa | 7.41±0.60(Predicted) |
Storage Condition | -20°C |
Use | LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis. Pre-clinically LY2090314 i stabilizes β-catenin and enhances the efficacy of platinum based regimens. |
Target | GSK-3α GSK-3β |
In vitro study | LY2090314 selectively inhibited the activity by GSK-3 by blocking ATP binding. LY2090314 is capable of stabilizing β-catenin. LY2090314 monotherapy showed limited efficacy. LY3090314 enhances the efficacy of cisplatin and carboplatin on solid tumor cancer cell lines in vitro. LY2090314 selectively inhibits the activity by GSK-3 by blocking ATP binding. LY2090314 is capable of stabilizing β-catenin. LY2090314 monotherapy showed limited efficacy. LY3090314 enhances the efficacy of cisplatin and carboplatin on solid tumor cancer cell lines in vitro. |
In vivo study | LY3090314 enhances the efficacy of cisplatin and carboplatin on solid tumor cancer cell lines in vitro. LY2090314 enhances the efficacy of cisplatin and carboplatin in xenografted solid tumors. |
Reference Show more | 1. Zamek-Gliszczynski MJ, et al. Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. Dr2. Atkinson JM, et al. Activating the Wnt/β-Catenin Pathway for the Treatment of Melanoma--Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3. PLoS One. 2015 Apr 27;10(4):e0125028. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.951 ml | 9.756 ml | 19.511 ml |
5 mM | 0.39 ml | 1.951 ml | 3.902 ml |
10 mM | 0.195 ml | 0.976 ml | 1.951 ml |
5 mM | 0.039 ml | 0.195 ml | 0.39 ml |