3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide
- Product Name
- 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide
- CAS No.
- 1232410-49-9
- Chemical Name
- 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide
- Synonyms
- VE-821;AVE821;CS-634;VE821;VE 821;ATR Inhibitor IV;VE-821;VE821;VE 821;VE-821 VE821 ATR Inhibitor IV;3-Amino-6-[4-(methlsulfonyl)phenyl)-N-phenyl-2-pyrazinecarboxamide;3-Amino-6-(4-methanesulfonylphenyl)-N-phenylpyrazine-2-carboxamide;3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
- CBNumber
- CB52534719
- Molecular Formula
- C18H16N4O3S
- Formula Weight
- 368.41
- MOL File
- 1232410-49-9.mol
3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide Property
- Melting point:
- 247-249°C
- Boiling point:
- 568.4±50.0 °C(Predicted)
- Density
- 1.394
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (40 mg/ml)
- pka
- 9.97±0.70(Predicted)
- form
- powder
- color
- white to beige
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
N-Bromosuccinimide Price
- Product number
- 5.04972
- Product name
- ATR Inhibitor IV - CAS 1232410-49-10 - Calbiochem
- Packaging
- 10mg
- Price
- $252
- Updated
- 2024/03/01
- Product number
- SML1415
- Product name
- VE-821
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $115
- Updated
- 2023/06/20
- Product number
- SML1415
- Product name
- VE-821
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $451
- Updated
- 2023/06/20
- Product number
- 17587
- Product name
- VE-821
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 17587
- Product name
- VE-821
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide Chemical Properties,Usage,Production
Description
Ataxia-telangiectasia and Rad3-related protein (ATR) is a serine/threonine kinase that activates DNA processes related to the DNA damage response. VE-821 is an ATP-competitive inhibitor of ATR (IC50 = 26 nM). It augments DNA damage and cell death of cancer cells in response to radiation under normal and hypoxic conditions. VE-821 also sensitizes cancer cells to chemotherapy.
Chemical Properties
Bright Yellow Solid
Uses
VE-821 has been used as an inhibitor of ATM- and Rad3-related (ATR) protein in human cancer cells.
Uses
VE 821 is a potent and selective inhibitor of DNA damage response kinase, ATR. VE 821 functions to disrupt DNA damage repair system of tumor cells, limiting their abilities for further growth.
Definition
ChEBI: 3-amino-6-(4-methylsulfonylphenyl)-N-phenyl-2-pyrazinecarboxamide is an aromatic amide.
Biochem/physiol Actions
VE-821 is a potent ATP-competitive inhibitor of the DNA damage response (DDR) kinase Ataxia telangiectasia-mutated (ATM) and ATM- and Rad3-related (ATR) with a Ki of 13 nM. VE-821 has minimal cross-reactivity against the related PIKKs ATM, DNA-dependent protein kinase (DNA-PK), mTOR and PI3-kinase-γ (Ki of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases. VE-821 used alone caused death in a large fraction of cancer cell populations and also showed strong synergy with genotoxic agents. VE-821 increased sensitivity of cells to radiation and also sensitized cancer cells to a variety of chemotherapeutic agents.
storage
Store at -20°C
References
Reaper et al. (2011), Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR; Nat. Chem. Biol., 7 428 Prevo et al. (2012), The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy; Cancer Biol. Ther., 13 1072 Huntoon et al. (2013), ATR inhibition broadly sensitizes ovarian cancer cells to chemotherapy independent of BRCA status; Cancer Res., 73 3683 King et al. (2021), Increased Replication Stress Determines ATR Inhibitor Sensitivity in Neuroblastoma Cells; Cancers (Basel), 13 6215 Moolmuang and Ruchirawat (2021), The antiproliferative effects of ataxia-telangiectasia mutated and ATM- and Rad3-related inhibitions and their enhancements with the cytotoxicity of DNA damaging agents in cholangiocarcinoma cells; J. Pharm. Pharmacol., 73 40
3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide manufacturers
- Product
- 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide 1232410-49-9
- Price
- US $1.00/KG
- Min. Order
- 1G
- Purity
- 98%
- Supply Ability
- 100KG
- Release date
- 2018-08-21