VX-984

VX-984

• CAS Number: 1476074-39-1
• UNSPSC Description: VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium[1][2][3].
• Target Antigen: DNA-PK
• Type: Isotope-Labeled Compounds
• Related Pathways: Cell Cycle/DNA Damage;PI3K/Akt/mTOR
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Purity: 98.86
• Solubility: DMSO : 10 mg/mL (ultrasonic)
• Smiles: O=C(C1=CC=NC2=C([C@H](C)CNC3=CC(C4=C([2H])N=C(C)N=C4[2H])=NC=N3)C=CC=C12)NC
• Molecular Weight: 415.49
• References & Citations: [1]Timme CR, et al. The DNA-PK Inhibitor VX-984 Enhances the Radiosensitivity of Glioblastoma Cells Grown In Vitro and as Orthotopic Xenografts. Mol Cancer Ther. 2018 Jun;17(6):1207-1216.|[2]Khan AJ, et al. VX-984 is a selective inhibitor of non-homologous end joining, with possible preferential activity in transformed cells. Oncotarget. 2018 May 25;9(40):25833-25841. |[3]Diane Boucher, et al. Abstract 3716: Potent radiation enhancement with VX-984, a selective DNA-PKcs inhibitor for the treatment of NSCLC. Cancer Res (2016) 76 (14_Supplement): 3716.|[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
• Shipping Conditions: Room Temperature
• Storage Conditions: -20°C, 3 years; 4°C, 2 years (Powder)
• Clinical Information: Phase 1