GW 806742X

GW 806742X is an inhibitor of necroptosis. It binds to mixed lineage kinase domain-like protein (Mlkl, Kd = 9.3 µM for the mouse protein), reducing its association with the cytoplasmic membrane, and decreases necroptosis induced by TNF-alpha, a Smac mimetic, and the caspase inhibitor Q-VD-OPH (Cay-15260) in isolated mouse dermal fibroblasts when used at a concentration of 500 nM. GW 806742X is also an inhibitor of VEGFR2 (IC50 = 2 nM). It decreases VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs, IC50 = 5 nM). GW 806742X (10 µM) inhibits mammosphere formation by, reduces the number of extracellular actin fibers extruding from, and decreases intracellular IL-1beta levels in, MDA-MB-231 triple-negative breast cancer cells.Formal Name: 3-[[4-[methyl[4-[[[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]phenyl]amino]-2-pyrimidinyl]amino]-benzenesulfonamide. CAS Number: 579515-63-2. Molecular Formula: C25H22F3N7O4S. Formula Weight: 573.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 10 mg/ml, Ethanol: 20 mg/ml. SMILES: O=C(NC1=CC=C(N(C)C2=NC(NC3=CC=CC(S(=O)(N)=O)=C3)=NC=C2)C=C1)NC4=CC=C(C=C4)OC(F)(F)F. InChi Code: InChI=1S/C25H22F3N7O4S/c1-35(22-13-14-30-23(34-22)31-18-3-2-4-21(15-18)40(29,37)38)19-9-5-16(6-10-19)32-24(36)33-17-7-11-20(12-8-17)39-25(26,27)28/h2-15H,1H3,(H2,29,37,38)(H,30,31,34)(H2,32,33,36). InChi Key: SNRUTMWCDZHKKM-UHFFFAOYSA-N.