Berzosertib (VE-822)

For research use only. Not for use in humans.

Catalog No.S7102 Synonyms: VX970,M6620

34 publications

Berzosertib (VE-822) Chemical Structure

Molecular Weight(MW): 463.55

VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.

Size Price Stock Quantity  
USD 147 In stock
USD 470 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Berzosertib (VE-822) has been cited by 34 publications

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.
Features The first ATR-targeted drug candidate with high selectivity for ATR.
Targets
ATR [1]
(HT29 cells)
19 nM
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCK1T-HPV16 NFPXWIhHfW6ldHnvckBCe3OjeR?= NF7iTmQxNjVibl2= MX2yOEBpyqB? NWnKTIFvcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gSVE> NF30N|YzPTdzN{GwPC=>
HCK1T-HPV16 MljaSpVv[3Srb36gRZN{[Xl? MUOwMlUhdk1? Mkj2NlQhcMLi NW\FRnJo\W6qYX7j[ZMhTTFvZHXw[Y5l\W62IILldIxq[2G2aX;uJI9nKHSqZTDIVHYyPiCpZX7vcYU> NIjLdWczPTdzN{GwPC=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / AKT / p-AKT; 

PubMed: 29890208     


VE-822 treatment inhibited STAT3-AKT pathway activation in both KYSE70 and KYSE450.

p21 / caspase-3 / PARP / γ-H2AX; 

PubMed: 29890208     


Expression of several markers which reflects the cell proliferation or cell apoptosis or cell cycle progression or DNA damage was examined using western blotting. Caspase-3 and cleaved-PARP expression remarkably increased in cells exposure to combination of VE-822 and cisplatin. In the ATMdeficient cell, VE-822 combination with cisplatin more dramatic changes in the expression of p-AKT, p21, and γ-H2AX than control cells.

PARP / RPA32 / γH2AX / H4 / MEK; 

PubMed: 31014753     


(A and B) THP-1 (Panel A) and MOLM-13 (Panel B) cells were treated with VE-822 and AZD1775, alone or in combination for 24 h. Chromatin-bound RPA32 and γH2AX were analyzed by western blotting and probed with the indicated antibodies.

WEE1 / p-CDC25c / p-CDK1 / CDK1 / p-CDK2 / CDK2 / RRM1 / RRM2; 

PubMed: 31014753     


THP-1 and MOLM-13 cells were treated with VE-822, AZD1775, or VE + AZD for 24 h. Whole cell lysates were subjected to western blotting and probed with the indicated antibodies. The fold changes for the densitometry measurements, normalized to GAPDH and compared to the untreated control, are shown below the corresponding blot.

29890208 31014753
Growth inhibition assay
Cell viability; 

PubMed: 31014753     


AML cells were cultured in 96-well plates with 0, 0.125, 0.25, 0.5, 1, and 2 µM VE-822 for 72 h and cells were incubated with MTT.

31014753
Immunofluorescence
PD-L1 / Hsp90B1; 

PubMed: 30094103     


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.

γH2AX / p53; 

PubMed: 29890208     


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.

30094103 29890208
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]
- Collapse
  • Animal Models: mice bearing PSN-1 or MiaPaCa-2 tumors
  • Formulation: saline
  • Dosages: 60 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (77.66 mM)
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
Formula

C24H25N5O3S
CAS No. 1232416-25-9
Storage powder
in solvent
Synonyms VX970,M6620
Smiles CNCC1=CC=C(C=C1)C2=NOC(=C2)C3=C(N)N=CC(=N3)C4=CC=C(C=C4)[S](=O)(=O)C(C)C

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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

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 )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

selleck catalog

ATM/ATR Signaling Pathway Map

Related ATM/ATR Products

  • AZD6738(Ceralasertib) New

    AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

  • Dorsomorphin (Compound C) New

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

  • KU-55933 (ATM Kinase Inhibitor)

    KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

  • VE-821

    VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.

  • KU-60019

    KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.

    Features:Improved analog of KU-55933, and is more effective at blocking ATM-mediated DDR events.

  • Chloroquine diphosphate

    Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

  • AZ20

    AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.

    Features:AZ20 is the first reported inhibitor of ATR protein kinase demonstrating tumor growth inhibition in vivo.

  • CP-466722

    CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.

  • ETP-46464

    ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.

    Features:Selective ATR inhibitor and particularly toxic to p53-deficient cancer cells. Often used as a pharmacologic probe due to its ideal pharmacological properties.

Tags: buy Berzosertib (VE-822) | Berzosertib (VE-822) supplier | purchase Berzosertib (VE-822) | Berzosertib (VE-822) cost | Berzosertib (VE-822) manufacturer | order Berzosertib (VE-822) | Berzosertib (VE-822) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID