LY-2090314 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 LY-2090314 i stabilizes β-catenin and enhances the efficacy of platinum based regimens.
CAS Number: 603288-22-8
Molecular Weight: 512.53
Chemical Name: 3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-4-(imidazo[1,2-a]pyridin-3-yl)-1H-pyrrole-2,5-dione
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 100 mg/mL(195.11 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
LY-2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY-2090314 is able to stabilize β-catenin. LY-2090314 shows limited efficacy as monotherapy. LY-3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro.
LY-2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts.
- Brail LH, et al. J Clin Oncol, 2011, 29, abstr 3030.
- A phase I dose-escalation, pharmacokinetic (PK), and pharmacodynamic (PD) evaluation of intravenous LY2090314 a GSK3 inhibitor administered in combination with pemetrexed and carboplatin. Meeting: 2011 ASCO Annual Meeting, Presenter: Les H. Brail.
Products are for research use only. Not for human use.
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