Home PI3K/Akt/mTOR ATM/ATR inhibitor Berzosertib (VE-822) For research use only.

Berzosertib (VE-822)

Synonyms: VX970, M6620

Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.

Berzosertib (VE-822) Chemical Structure

Berzosertib (VE-822) Chemical Structure

CAS No. 1232416-25-9

Purity & Quality Control

Products often used together with Berzosertib (VE-822)

Sacituzumab-govitecan

Berzosertib and Sacituzumab Govitecan demonstrate anti-tumor activity in heavily pre-treatment tumors.

Berg SA, et al. Clin Cancer Res. 2023;CCR-23-1422.

Berzosertib (VE-822) Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCK1T-HPV16 Function Assay 0.5 nM 24 h  enhances E1-dependent replication of the HPV16 genome 25717108
HCK1T-HPV16 Function Assay 0.5 nM 24 h  increases the levels of E1 25717108
MDCK Cytotoxicity assay 50 nM 72 h Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability at 50 nM pretreated for 72 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay 27823879
Click to View More Cell Line Experimental Data

Biological Activity

Description Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
Features The first ATR-targeted drug candidate with high selectivity for ATR.
Targets
ATR [1]
(HT29 cells)
19 nM
In vitro
In vitro

VE-822 (80 nM) attenuates ATR signaling pathway and reduces survival in tumor cells in response to XRT and LY-188011. VE-822 (80 nM) attenuates ATR signaling in normal cells without enhancing radiation and LY-188011 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 LY-188011 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]
Cell Research Cell lines HT29 cells
Concentrations 19 nM
Incubation Time 24 h
Method

Cells were treated with different concentrations of VE-822.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 / AKT / p-AKT p21 / caspase-3 / PARP / γ-H2AX PARP / RPA32 / γH2AX / H4 / MEK WEE1 / p-CDC25c / p-CDK1 / CDK1 / p-CDK2 / CDK2 / RRM1 / RRM2 29890208
Growth inhibition assay Cell viability 31014753
Immunofluorescence PD-L1 / Hsp90B1 γH2AX / p53 30094103
In Vivo
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 LY-188011 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]
Animal Research Animal Models mice bearing PSN-1 or MiaPaCa-2 tumors
Dosages 60 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02723864 Completed
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 August 9 2017 Phase 1
NCT02487095 Active not 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)
 July 30 2015 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 463.55 Formula

C24H25N5O3S
CAS No. 1232416-25-9 SDF Download Berzosertib (VE-822) SDF
Smiles CC(C)S(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C3=CC(=NO3)C4=CC=C(C=C4)CNC)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 23 mg/mL ( (49.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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Frequently Asked Questions

Question 1:
I want to have information to prepare VE-822 for mouse gavage. Thank you for your answer

Answer:
VE-822 can be dissolved in 1% CMC Na at 30mg/ml as a suspension for oral gavage.

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