Berzosertib (VE-822|VX970|M6620)
Catalog No.S7102 Synonyms: VX970
Molecular Weight(MW): 463.55
VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
6 Customer Reviews
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Western blot analysis of scr or siPNUTS transfected cells without IR or 6 h after 10 Gy. VE-822 was added for 2, 5, 15, 30 or 60 min to indicated samples 6 h after 10 Gy.
Nucleic Acids Res, 2018, doi:10.1093/nar/gky1233. Berzosertib (VE-822|VX970|M6620) purchased from Selleck.
Combination treatment enhanced the DNA damage effect presented by examining fluorescence intensity of γ-H2A.X and p53 in ESCC cells. Cells treated with cisplatin, VE-822, or combination of two drugs for 24 h were fixed and co-labeled with anti-γH2AX and anti-p53 antibodies. The γ-H2A.X and p53 foci were analyzed by immunofluorescence microscopy. Combination treatment resulted in accumulation of DNA damage presented by stronger and more fluorescence staining of γ-H2AX and p53.
Cancer Lett, 2018, 432:56-68. Berzosertib (VE-822|VX970|M6620) purchased from Selleck.
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Flow cytometry analysis of E14.5 FL lineage negative cells from indicated genotypes treated with ATMi (KU-55933; 1nM), ATRi (VE-822; 1nM) or both inhibitors or DMSO as a negative control for 24 hours in culture before AnnexinV and PI levels were measured.
Sci Rep, 2016, 6:27379.. Berzosertib (VE-822|VX970|M6620) purchased from Selleck.
Western blot analysis for a time course experiment in the presence of wortmannin (lanes 5 to 8), VE-822 (lanes 9 to 12), or a vehicle control (lanes 1 to 4).
J Virol, 2015, 89(9): 5040-59 . Berzosertib (VE-822|VX970|M6620) purchased from Selleck.
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The copy number of HPV16 genomes was measured by qPCR.
J Virol, 2015, 89(9): 5040-59 . Berzosertib (VE-822|VX970|M6620) purchased from Selleck.
HeLa-GFP-PD-L1 cells were treated with cisplatin (10 μM) for 24 hours with or without VE-822 (0.1 μM) pretreatment, and PD-L1 localization was analyzed by immunofluorescence.
Am J Cancer Res, 2018, 8(7):1307-1316. Berzosertib (VE-822|VX970|M6620) purchased from Selleck.
Purity & Quality Control
Choose Selective ATM/ATR Inhibitors
Biological Activity
| Description | VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells. | |||||||||||||||||||||||
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| Features | The first ATR-targeted drug candidate with high selectivity for ATR. | |||||||||||||||||||||||
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| In vitro |
VE-822 (80 nM) attenuates ATR signaling pathway and reduces survival in tumor cells in response to XRT and gemcitabine. VE-822 (80 nM) attenuates ATR signaling in normal cells without enhancing radiation and gemcitabine killing in normal cells. VE-822 (80 nM) increases XRT-induced residual γH2AX and 53BP1 foci compared with XRT in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) pre-treatment decreases Rad51 foci after XRT in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) alone increases the G1-phase-fraction in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) abrogates XRT enriched G2/M-phase-fraction in MiaPaCa-2 and PSN-1 cells. VE-822 has little effect alone, while VE-822 (80 nM) combined with XRT and/or gemcitabine enhances early and late apoptosis in PSN-1 cells that is strongest in the triple combination. [1] VE-822 increases tumor response to DNA damaging agents associated with blockade of pChk1 Ser345. [2] |
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| Cell Data |
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| In vivo | VE-822 (60 mg/kg) inhibits phospho-Ser-345-Chk1 in mice bearing PSN-1 tumors after DNA-damaging agents. VE-822 (60 mg/kg) combined with XTR doubles the time for tumors to grow to 600 mm3 of XRT alone in mice bearing both PSN-1 and MiaPaCa-2 tumors. VE-822 (60 mg/kg) added to the combination of gemcitabine and XRT substantially prolongs the tumor growth delay compared with the Gem+XRT1 group n mice bearing both PSN-1 tumors. VE-822 (60 mg/kg) combined with XRT1 increases uptake in tumors by 44% compared with XRT1, suggesting that addition of VE-822 increased γH2AX phosphorylation and persistence of DNA damage caused by XRT. [1] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 36 mg/mL (77.66 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+45% PEG 300+H2O For best results, use promptly after mixing. |
11mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 463.55 |
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| Formula | C24H25N5O3S |
| CAS No. | 1232416-25-9 |
| Storage | powder |
| in solvent | |
| Synonyms | VX970 |
Bio Calculators
Molarity Calculator
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02723864 | Recruiting | Neoplasms | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | August 9 2017 | Phase 1 |
| NCT02723864 | Recruiting | Neoplasms | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | August 9 2017 | Phase 1 |
| NCT02487095 | Recruiting | Carcinoma Non-Small -Cell Lung|Ovarian Neoplasms|Small Cell Lung Carcinoma|Uterine Cervical Neoplasms|Carcinoma Neuroendocrine|Extrapulmonary Small Cell Cancer | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | June 18 2015 | Phase 1|Phase 2 |
| NCT02487095 | Recruiting | Carcinoma Non-Small -Cell Lung|Ovarian Neoplasms|Small Cell Lung Carcinoma|Uterine Cervical Neoplasms|Carcinoma Neuroendocrine|Extrapulmonary Small Cell Cancer | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | June 18 2015 | Phase 1|Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
I want to have information to prepare VE-822 for mouse gavage. Thank you for your answer
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Answer:
VE-822 can be dissolved in 1% CMC Na at 30mg/ml as a suspension for oral gavage.
