VE-821 NEW
| Price | $46 | $72 | $126 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: VE-821 | CAS No.: 1232410-49-9 |
| Purity: 99.97% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | VE-821 |
| 描述 | VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki/IC50: 13/26 nM in cell-free assays). |
| 細胞實驗 | Clonogenic survival assays were performed as described before. Briefly, logarithmically growing cells were plated in triplicate in 6-well tissue culture dishes under oxic (21% O2) or hypoxic conditions (0.5% O2) using an InVivo2 300 chamber. Cells were incubated for 6 h before irradiation under oxia or hypoxia using tightly sealed chambers. The target O2 level was achieved within 6 h of gassing and maintained during irradiation, as confirmed by an OxyLite oxygen probe. Cells irradiated under hypoxia were exposed to normoxia at 1 h post-irradiation. As standard, VE-821 (1 μM) was added 1 h prior to irradiation (6 Gy) and was washed away 72 h after irradiation. For the chemotherapy experiments, cells were initially exposed to increasing concentrations of gemcitabine (5, 10 and 20 nM) for 24 h before addition of the VE-821 (1 μM) for another 72 h. The effect of triple combination of irradiation with VE-821 and gemcitabine was examined as well. Cells were incubated for 10–21 d until colonies were stained with 0.5% crystal violet and counted in a CellCount automated colony counter. Clonogenic survival was calculated and data were fitted in GraphPad Prism 4.0 [2]. |
| 激酶實驗 | The ability of compounds (e.g., VE-821) to inhibit ATR, ATM or DNAPK kinase activity is tested using a radiometric-phosphate incorporation assay. A stock solution is prepared consisting of the appropriate buffer, kinase, and target peptide. To this is added the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [g-33P]ATP solution and incubated at 25°C. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66 μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared, and washed six times with 200 μL of 100 mM phosphoric acid, prior to the addition of 100 μL of scintillation cocktail and scintillation counting on a 1450 Microbeta Liquid Scintillation Counter. Dose-response data are analyzed using GraphPad Prism software [4]. |
| 體外活性 | VE-821 exhibits high selectivity for ATR with minimal cross-reactivity against related PIKKs, including ATM, DNA-dependent protein kinase (DNA-PK), mammalian target of rapamycin, and phosphoinositol 3-kinase-γ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively). It inhibits H2AX phosphorylation in hydroxyurea-treated HT29 cancer cells without affecting M059J or HT144 lines treated with neocarzinostatin [1]. VE-821 significantly increases the sensitivity of PSN-1, MiaPaCa-2, and primary PancM pancreatic cancer cells to radiation and gemcitabine under both normoxic and hypoxic conditions, leading to the inhibition of radiation-induced G2/M arrest [2]. Additionally, VE-821 (1 and 4 μM) enhances H2AX phosphorylation at Ser139 in OVCAR-8 cells induced by topotecan and cisplatin but does not block ATR-mediated Ser345 Chk1 or Ser296 autophosphorylation induced by gemcitabine, topotecan, or cisplatin [3]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 69 mg/mL (187.3 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 關鍵字 | VE-821 | ATM and RAD3 related | VE 821 | ATM/ATR | Inhibitor | Ataxia telangiectasia mutated | inhibit | VE821 |
| 相關產(chǎn)品 | CP-466722 | Ro 90-7501 | Dactolisib | Berzosertib | Elimusertib | GJ103 sodium salt | KU60019 | Ceralasertib | (Z)-Mirin | NU6027 | Schisandrin B | AZ32 |
| 相關庫 | 抗肺癌化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗癌細胞代謝庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 臨床前化合物庫 | 抗癌活性化合物庫 | 氧化還原化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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