GSK215

GSK215 is a proteolysis-targeting chimera (PROTAC) composed of the focal adhesion kinase (FAK) inhibitor PND1186 (Cay-17668) linked to the von-Hippel Lindau (VHL) E3 ligase ligand VHL-021. It binds to the FAK kinase domain (IC50 = 15.8 nM) and induces FAK degradation in A549 lung cancer cells with a 50% degradation concentration (DC50) of 1.3 nM. GSK215 (100 nM) inhibits A549 cell migration and invasion. In vivo, GSK215 (8 mg/kg) reduces hepatic FAK levels in mice.Formal Name: (2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide. CAS Number: 2743427-26-9. Molecular Formula: C50H59F3N10O6S. Formula Weight: 985.1. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly Soluble: 1-10 mg/ml, Ethanol: Soluble: >10 mg/ml. SMILES: FC(F)(C(C(NC(C=CC=C1)=C1C(NC)=O)=C2)=CN=C2NC(C=CC(N(CC3)CCN3CC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=C7)=C7OC)F. InChi Code: InChI=1S/C50H59F3N10O6S/c1-29(31-12-14-32(15-13-31)44-30(2)56-28-70-44)57-47(67)40-23-34(64)26-63(40)48(68)45(49(3,4)5)60-43(65)27-61-18-20-62(21-19-61)33-16-17-38(41(22-33)69-7)59-42-24-39(36(25-55-42)50(51,52)53)58-37-11-9-8-10-35(37)46(66)54-6/h8-17,22,24-25,28-29,34,40,45,64H,18-21,23,26-27H2,1-7H3,(H,54,66)(H,57,67)(H,60,65)(H2,55,58,59)/t29-,34+,40-,45+/m0/s1. InChi Key: ZGSWGXNEXAXEGV-XFCHVEHOSA-N.