Stereochemistry | ACHIRAL |
Molecular Formula | C28H25FN6O3 |
Molecular Weight | 512.5349 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC2=C3N(CCN(C2)C(=O)N4CCCCC4)C=C(C3=C1)C5=C(C(=O)NC5=O)C6=CN=C7C=CC=CN67
InChI
InChIKey=HRJWTAWVFDCTGO-UHFFFAOYSA-N
InChI=1S/C28H25FN6O3/c29-18-12-17-15-34(28(38)32-7-3-1-4-8-32)11-10-33-16-20(19(13-18)25(17)33)23-24(27(37)31-26(23)36)21-14-30-22-6-2-5-9-35(21)22/h2,5-6,9,12-14,16H,1,3-4,7-8,10-11,15H2,(H,31,36,37)
LY-2090314 is a GSK-3alpha and GSK-3beta inhibitor developed by Eli Lilly. Phase 2 clinical trials of LY-2090314 as a signle agenst against acute leukemia did not show clinical benefit. LY-2090314 was studied in combination pemetrexed and carboplatin against solid tumors, and in combination with FOLFOX, gemcitabine, and nab-paclitaxel against pancreatic cancer.
Originator
Approval Year
Sourcing
Sample Use Guides
In clinical trial agaisnt AML 40mg LY2090314 was administered intravenously on days 1, 8 and 15 of a 28 day cycle.
Route of Administration:
Intravenous
Inhibition of GSK3-alpha was determined in biochemical assay. A standard filter binding protocol was used measuring the ability of recombinant GSK3-alpha to phosphorylate phospho-CREB (cAMP response element binding protein) at serine-129 with ATP[gamma-33P] in the presence of test compound.