VX-984

VX-984 is an inhibitor of DNA protein kinase (DNA-PK). It inhibits radiation-induced increases in phosphorylated DNA-PK levels in U251 and NSC11 glioblastoma cells when used at concentrations of 250 or 500 nM. VX-984 (1 µM) induces mutagenic NHEJ and homologous recombination DNA repair pathways in a reporter assay using U2OS cells. It potentiates radiation-induced cytotoxicity and DNA damage in U251 and NSC11 cells when used at concentrations of 250 or 500 nM. In vivo, VX-984 (50 mg/kg twice per day), in combination with radiation, increases survival in a U251 orthotopic mouse xenograft model.Formal Name: N-methyl-8-[(1S)-1-methyl-2-[(2'-methyl[4,5'-bipyrimidin]-6-yl-4',6'-d2)amino]ethyl]-4-quinolinecarboxamide. CAS Number: 1476074-39-1. Synonyms: M-9831. Molecular Formula: C23H21D2N7O. Formula Weight: 415.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: CC1=NC([2H])=C(C([2H])=N1)C2=CC(NC[C@@H](C)C3=CC=CC4=C3N=CC=C4C(NC)=O)=NC=N2. InChi Code: InChI=1S/C23H23N7O/c1-14(17-5-4-6-18-19(23(31)24-3)7-8-25-22(17)18)10-28-21-9-20(29-13-30-21)16-11-26-15(2)27-12-16/h4-9,11-14H,10H2,1-3H3,(H,24,31)(H,28,29,30)/t14-/m1/s1/i11D,12D. InChi Key: PEACIOGDEQRHFA-KIYKJNLWSA-N.