LY-2090314

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.

Product information

CAS Number: 603288-22-8

Molecular Weight: 512.53

Formula: C28H25FN6O3

Synonym:

LY 2090314

LY2090314

LY-2090314

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

Smiles: O=C1NC(=O)C(=C1C1=CN=C2C=CC=CN21)C1C=CC2CNC(CN3C(F)=CC=1C3=2)C(=O)N1CCCCC1

InChiKey: FWWMRDPEXYCBRS-UHFFFAOYSA-N

InChi: InChI=1S/C28H25FN6O3/c29-21-12-18-17(23-24(27(37)32-26(23)36)20-14-31-22-6-2-5-11-34(20)22)8-7-16-13-30-19(15-35(21)25(16)18)28(38)33-9-3-1-4-10-33/h2,5-8,11-12,14,19,30H,1,3-4,9-10,13,15H2,(H,32,36,37)

Technical Data

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

In Vitro:

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.

In Vivo:

LY-2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts.

References:

1. Brail LH, et al. J Clin Oncol, 2011, 29, abstr 3030.
2. 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.