VE-821

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、ATP 竞争性的 ATR 抑制剂，Ki/IC50 为 13 nM/26 nM；与相关 PIKKs ATM、DNA-PK、mTOR 和 PI3K 相比，ATR 表现出优异的选择性。

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.

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.

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VE821 | VE 821

Cell Cycle/DNA Damage

ATM/ATR

ATR

Cancer

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1232410-49-9

368.4096

C18H16N4O3S

>98% (HPLC)

10 mM in DMSO

O=C(C1=NC(C2=CC=C(S(=O)(C)=O)C=C2)=CN=C1N)NC3=CC=CC=C3

2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-

(-20℃)

With Ice Pack

≥ 2 years