product name LY2090314
Description: LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; it may improve the efficacy of platinum-based chemotherapy regimens. Pre-clinically LY2090314 stabilizes β-catenin and enhances the efficacy of platinum based regimens. With limited predicted efficacy as monotherapy, this first in human study was conducted in combination with pemetrexed+ carboplatin (PC). LY2090314 at 40 mg can be safely combined with PC. At these exposures, β-catenin is up-regulated and the adverse event profile is acceptable.
References: Brail LH, et al. J Clin Oncol, 2011, 29, abstr 3030.
512.53
Formula
C28H25FN6O3
CAS No.
603288-22-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (195.1 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL warmed (3.9 mM)
Solubility (In vivo)
Synonyms
LY 2090314; LY-2090314
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423999
| In Vitro |
In vitro activity: LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY2090314 is able to stabilize β-catenin. LY2090314 shows limited efficacy as monotherapy. LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts |
| Animal model | |
| Formulation & Dosage | |
| References | [1] Brail LH, et al. J Clin Oncol, 2011, 29, abstr 3030. |
