"目錄號: HY-14731
Cell Cycle/DNA DamagePI3K/Akt/mTOR-
VE-821 是一種有效的 ATP 競爭性的ATR抑制劑，Ki/IC50為 13 nM/26 nM。
相關(guān)產(chǎn)品
Wortmannin-AZD6738-VE-822-KU-55933-KU-60019-AZD0156-CP-466722-AZ20-CGK733-ETP-46464-HLM006474-BAY-1895344 hydrochloride-
生物活性
Description
VE-821 is a potent ATP-competitive inhibitor ofATRwithKi/IC50of 13 nM/26 nM.
IC50& Target
Ki: 13 nM (ATR)[1]
IC50: 26 nM (ATR)[2]
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[1]. VE-821 also inhibits ATM and DNA-PK wirh IC50of >8 μM, and 4.4 μM, respectively[2]. 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[3].
References
