VE-821

SKU: orb1226720

Description

A potent, selective and ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM; shows excellent selectivity for ATR over the related PIKKs ATM, DNA-PK, mTOR and PI3K.

Key Properties

• CAS Number: 1232410-49-9
• MW: 368.4096
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₆N₄O₃S
• SMILES: O=C(C1=NC(C2=CC=C(S(=O)(C)=O)C=C2)=CN=C1N)NC3=CC=CC=C3
• Target: ATM/ATR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3Kγ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases. VE-821 (compound 27) also inhibits ATM and DNA-PK wirh IC50 of >8 μM, and 4.4 μM, respectively. VE-821 significantly enhances the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and Gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 leads to inhibition of radiation-induced G2/M arrest in cancer cells. In both PSN-1 and MiaPaCa-2 cells, 1 μM VE-821 inhibits phosphorylation of Chk1 (Ser 345) after treatment with Gemcitabine (100 nM), radiation (6 Gy) or both, at 2 h post-irradiation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

VE821 | VE 821

Quick Database Links

Gene Symbol

ATM/ATR