VE 821

Pricing Availability   Qty
Description: High affinity and selective ATP-competitive ATR inhibitor
Chemical Name: 3-Amino-6-[4-(methlsulfonyl)phenyl)-N-phenyl-2-pyrazinecarboxamide
Purity: ≥98% (HPLC)
Literature (4)

Biological Activity for VE 821

VE 821 is a high affinity and selective ATP-competitive ATR inhibitor (Ki = 13 nM). Exhibits >75-fold selectivity for ATR over related kinases mTOR, DNA-PK, PI 3-Kγ and PIKKs (Ki values are >1, 2.2, 3.9 and 16 μM, respectively) and a panel of other kinases. Induces cell death in colon cancer cell lines in vitro and sensitizes tumor cells to treatment with DNA damaging anticancer agents.

Technical Data for VE 821

M. Wt 368.41
Formula C18H16N4O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1232410-49-9
PubChem ID 51000408
Smiles CS(=O)(C1=CC=C(C2=NC(C(NC3=CC=CC=C3)=O)=C(N=C2)N)C=C1)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for VE 821

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 36.84 100

Preparing Stock Solutions for VE 821

The following data is based on the product molecular weight 368.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.71 mL 13.57 mL 27.14 mL
5 mM 0.54 mL 2.71 mL 5.43 mL
10 mM 0.27 mL 1.36 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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References for VE 821

References are publications that support the biological activity of the product.

Reaper et al (2011) Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat.Chem.Biol. 7 428 PMID: 21490603

Williamson et al (2016) ATR inhibitors as a synthetic lethal therapy for tumours deficient in ARID1A. Nat.Commun. 7 13837 PMID: 27958275

If you know of a relevant reference for VE 821, please let us know.

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Citations for VE 821

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Currently there are no citations for VE 821. Do you know of a great paper that uses VE 821 from Tocris? Please let us know.

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