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Berzosertib (VE-822)

Name: Berzosertib (VE-822)
Brand: Selleck Chemicals
SKU: S7102
Rating: 5 (139 reviews)

Synonyms: VX970, M6620

Catalog No.S7102 Purity:99.33%

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

Berzosertib (VE-822) Chemical Structure

CAS No. 1232416-25-9

Purity & Quality Control

Batch: Purity: 99.33%

99.33

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

Related Targets	ATM ATR	Click to Expand
Related Products	KU-55933 VE-821 KU-60019 Ceralasertib (AZD6738) AZ20 AZD0156 Mirin AZD1390 CP-466722 Elimusertib (BAY-1895344) hydrochloride ETP-46464 Elimusertib (BAY-1895344) CGK 733 VX-803 (M4344) AZ31 AZ32 HAMNO	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

ATM/ATR Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 450 μL PEG 300, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (3.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then Continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
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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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