VE-821
CAS No. : 1232410-49-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $55 | In-stock |
| 10mg | $94 | In-stock |
| 25mg | $165 | In-stock |
| 50mg | $275 | In-stock |
| 100mg | $495 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-14731 |
| M.Wt: | 368.41 |
| Formula: | C18H16N4O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (ultrasonic);H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) |
VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 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 (compound 27) also inhibits ATM and DNA-PK wirh IC50 of >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].
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