An inhibitor of ATR
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VE-821

Item No. 17587

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide
CAS Number
1232410-49-9
Synonyms
  • ATR Inhibitor IV
Molecular Formula
C18H16N4O3S
Formula Weight
368.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 20 mg/ml
λmax
224, 304, 382 nm
SMILES
O=C(C1=NC(C2=CC=C(S(C)(=O)=O)C=C2)=CN=C1N)NC3=CC=CC=C3
InChi Code
InChI=1S/C18H16N4O3S/c1-26(24,25)14-9-7-12(8-10-14)15-11-20-17(19)16(22-15)18(23)21-13-5-3-2-4-6-13/h2-11H,1H3,(H2,19,20)(H,21,23)
InChi Key
DUIHHZKTCSNTGM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $186

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    Product Description

    VE-821 is an ATP-competitive inhibitor of ATR (IC50 = 26 nM).1,2 It augments DNA damage and cell death of cancer cells in response to radiation under normal and hypoxic conditions.2,3,4 VE-821 also sensitizes cancer cells to chemotherapy.3,5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Reaper, P.M., Griffiths, M.R., Long, J.M., et al. Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat. Chem. Biol. 7(7), 428-430 (2011).

    2. Pires, I.M., Olcina, M.M., Anbalagan, S., et al. Targeting radiation-resistant hypoxic tumour cells through ATR inhibition. Br. J. Cancer 107, 291-299 (2012).

    3. Prevo, R., Fokas, E., Reaper, P.M., et al. The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy. Cancer Biol. Ther. 13(11), 1072-1081 (2012).

    4. Salovská, B., Fabrik, I., Durisová, K., et al. Radiosensitization of human leukemic HL-60 cells by ATR kinase inhibitor (VE-821): Phosphoproteomic analysis. Int. J. Mol. Sci. 15, 12007-12026 (2014).

    5. Huntoon, C.J., Flatten, K.S., Wahner Hendrickson, A.E., et al. ATR inhibition broadly sensitizes ovarian cancer cells to chemotherapy independent of BRCA status. Cancer Res. 73(12), 3683-3691 (2013).

    6. Flynn, R.L., Cox, K.E., Jeitany, M., et al. Alternative lengthening of telomeres renders cancer cells hypersensitive to ATR inhibitors. Science 347(6219), 273-277 (2015).