bs-60317C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 442.51

Formula: C17 H11 K N2 O6 S2

CAS Number: 1956356-56-1

InChi Key: PHUNRLYHXGMOLG-WQRRWHLMSA-M

InChi: InChI=1S/C17H12N2O6S2.K/c20-15(21)7-8-18-16(22)14(27-17(18)26)9-12-5-6-13(25-12)10-1-3-11(4-2-10)19(23)24;/h1-6,9H,7-8H2,(H,20,21);/q;+1/p-1/b14-9-;

Smiles: [K+].[O-]C(=O)CCN1C(=O)/C(=C/C2=CC=C(O2)C2C=CC(=CC=2)[N+]([O-])=O)/SC1=S

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 ~0.75 µM (TOPflash assay). It binds directly to the regulators of G-protein signaling domain of axin, initiating β-catenin and Ras degradation through enhancement of the β-catenin destruction complex activating GSK3β. KYA1797K can effectively suppress the growth of CRCs harboring APC and KRAS mutations, as shown by various in vitro studies and by in vivo studies using xenograft and transgenic mouse models of tumors induced by APC and KRAS mutations. Destabilization of both β-catenin and Ras via targeting axin is a potential therapeutic strategy for treatment of CRC and other type cancers activated Wnt/β-catenin and Ras pathways.