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VE-821
| Product Name | VE-821 |
| Price: | Inquiry |
| Catalog No.: | CN00559 |
| CAS No.: | 1232410-49-9 |
| Molecular Formula: | C18H16N4O3S |
| Molecular Weight: | 368.4 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(c1nc(cnc1N)c1ccc(cc1)S(=O)(=O)C)Nc1ccccc1 |
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| Description | VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM. |
| Target | ATR:13 nM (Ki) ATM:16 μM (Ki) DNA-PK:2.2 μM (Ki) PI3Kγ:3.9 μM (Ki) |
| 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]. |
| Cell Assay | MiaPaCa-2, PSN-1 and Panc1 cells (5×104) are plated in 96-well plates and after 4 h treated with increasing concentrations of VE-821 at 1 h before irradiation with a single dose of 4 Gy. Medium is replaced 72 h post-irradiation at which point viability is measured using the using the Alamar Blue assay. Cells are allowed to proliferate and cell viability is again analyzed at day 10 for the different treatment conditions. Cell viability and surviving fraction are normalized to the untreated (control) group[3]. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 568.4±50.0 °C at 760 mmHg |
| Flash Point | 297.6±30.1 °C |
| Exact Mass | 368.094299 |
| PSA | 126.91000 |
| LogP | 2.93 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Storage condition | -20°C |