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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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V125220-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $53.90 | |
V125220-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $162.90 | |
V125220-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $489.90 |
Potent, selective ATP competitive ATR inhibitor
Synonyms | VE-821 | 1232410-49-9 | 3-Amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide | VE 821 | VE821 | 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide | CHEMBL1766779 | 3-amino-6-(4-methylsulfonylphenyl)-N-phenylpyrazine-2-carboxamide | BF884T |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | VE-821 is a novel ATR inhibitor. VE-821, sensitises tumour cells to DNA damage induced by radiation or chemotoxic drugs, by disrupting the DNA damage checkpoint and inhibiting DNA repair.Potent, selective ATP competitive ATR inhibitor (K i\xa0= 13 nM). Ex |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of ATR serine/threonine kinase |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | 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. |
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IUPAC Name | 3-amino-6-(4-methylsulfonylphenyl)-N-phenylpyrazine-2-carboxamide |
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INCHI | InChI=1S/C18H16N4O3S/c1-26(24,25)14-9-7-12(8-10-14)15-11-20-17(19)16(22-15)18(23)21-13-5-3-2-4-6-13/h2-11H,1H3,(H2,19,20)(H,21,23) |
InChi Key | DUIHHZKTCSNTGM-UHFFFAOYSA-N |
Canonical SMILES | CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N |
Isomeric SMILES | CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N |
PubChem CID | 51000408 |
Molecular Weight | 368.41 |
PubChem CID | 51000408 |
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CAS Registry No. | 1232410-49-9 |
ChEMBL Ligand | CHEMBL1766779 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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E1712148 | Certificate of Analysis | Jan 16, 2023 | V125220 |
Solubility | DMSO 74 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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1. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu. (2023) PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma. CANCER RESEARCH, 83 (7): (1094-1110). [PMID:36696363] |
1. Reaper PM, Griffiths MR, Long JM, Charrier JD, Maccormick S, Charlton PA, Golec JM, Pollard JR. (2011) Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR.. Nat Chem Biol, 7 (7): (428-30). [PMID:21490603] |
2. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu. (2023) PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma. CANCER RESEARCH, 83 (7): (1094-1110). [PMID:36696363] |