An inhibitor of DNA-PK
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VX-984

Item No. 42072

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    VX-984 is an inhibitor of DNA protein kinase (DNA-PK).1 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.2 It potentiates radiation-induced cytotoxicity and DNA damage in U251 and NSC11 cells when used at concentrations of 250 or 500 nM.1 In vivo, VX-984 (50 mg/kg twice per day), in combination with radiation, increases survival in a U251 orthotopic mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Timme, C.R., Rath, B.H., O-Neill, J.W., et al. The DNA-PK inhibitor VX-984 enhances the radiosensitivity of glioblastoma cells grown in vitro and as orthotopic xenografts. Mol. Cancer Ther. 17(6), 1207-1216 (2018).

    2. Khan, A.J., Misenko, S.M., Thandoni, A., et al. VX-984 is a selective inhibitor of non-homologous end joining, with possible preferential activity in transformed cells. Oncotarget 9(40), 25833-25841 (2018).