LY2090314

DESCRIPTION

A potent and selective inhibitor of GSK3 (IC50s = 1.5 and 0.9 for human recombinant GSK3α and GSK2β, respectively); has >10-fold selectivity for GSK3 against a panel of 40 kinases at a concentration of 20 μM; induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro; has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines (IC50s = 430 to >20,000 nM); knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro; reduces tumor volume in a murine A375 xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect

DETAILS

Inchi: 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)
Purity: ≥98%
Raptas: Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|GSK3 Signaling||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling
Smiles: O=C(N1)C(C2=CN=C3N2C=CC=C3)=C(C4=CN5C6=C4C=C(F)C=C6CN(C(N7CCCCC7)=O)CC5)C1=O
Inchikey: HRJWTAWVFDCTGO-UHFFFAOYSA-N
Cas Number: 603288-22-8
Formulation: A crystalline solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C28H25FN6O3
Formula Weight: 512.5
Shelf Life Days: 1460