VX-984
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].
Product Specifications
CAS Number
1476074-39-1
Product Name Alternative
M9831
UNSPSC
12352005
Target
DNA-PK
Type
Isotope-Labeled Compounds
Related Pathways
Cell Cycle/DNA Damage; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Purity
99.47
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 Formula
C23H21D2N7O
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)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
Phase 1
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