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Formula | C18H16N4O3S |
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Molecular Weight | 368.41 | CAS No. | 1232410-49-9 | ||||
Solubility (25°C)* | In vitro | DMSO | 74 mg/mL (200.86 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | VE-821(ATR inhibitor IV) 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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In vitro | VE-821(ATR inhibitor IV) shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3K (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. VE-821 alone commits a large fraction of cancer cell populations to death, but it only reversibly limits cell cycle progression in normal cells, with minimal death or long-term detrimental effects. [1] VE-821(ATR inhibitor IV) inhibits H2AX cell growth with IC50 of 800 nM. [2] |
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In vivo | VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR. |
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Data from [Data independently produced by Toxicol Sci, 2014, 10.1093/toxsci/kfu207]
Data from [Data independently produced by J Biol Chem, 2014, 289(35), 24314-24]
Data from [Data independently produced by , , Nature, 2018, 555(7696):387-391]
Data from [Data independently produced by , , Cancer Res, 2017, 77(17):4567-4578]
The thioredoxin system determines CHK1 inhibitor sensitivity via redox-mediated regulation of ribonucleotide reductase activity [ Nat Commun, 2024, 15(1):4667] | PubMed: 38821952 |
Comprehensive multi-omics analysis reveals WEE1 as a synergistic lethal target with hyperthermia through CDK1 super-activation [ Nat Commun, 2024, 15(1):2089] | PubMed: 38453961 |
Immunomodulatory effects and improved outcomes with cisplatin- versus carboplatin-based chemotherapy plus atezolizumab in urothelial cancer [ Cell Rep Med, 2024, 5(2):101393] | PubMed: 38280376 |
ATR limits Rad18-mediated PCNA monoubiquitination to preserve replication fork and telomerase-independent telomere stability [ EMBO J, 2024, 43(7):1301-1324] | PubMed: 38467834 |
DNA damage remodels the MITF interactome to increase melanoma genomic instability [ Genes Dev, 2024, 38(1-2):70-94] | PubMed: 38316520 |
Mechanism of Musashi2 affecting radiosensitivity of lung cancer by modulating DNA damage repair [ MedComm (2020), 2024, 5(5):e548] | PubMed: 38645664 |
Irradiated tumour cell-derived microparticles upregulate MHC-I expression in cancer cells via DNA double-strand break repair pathway [ Cancer Lett, 2024, 592:216898] | PubMed: 38670306 |
The ARID1A-METTL3-m6A axis ensures effective RNase H1-mediated resolution of R-loops and genome stability [ Cell Rep, 2024, 43(2):113779] | PubMed: 38358891 |
RAD51 separation of function mutation disables replication fork maintenance but preserves DSB repair [ iScience, 2024, 27(4):109524] | PubMed: 38577109 |
New insights into ATR inhibition in muscle invasive bladder cancer: The role of apolipoprotein B mRNA editing catalytic subunit 3B [ Oncol Res, 2024, 32(6):1021-1030] | PubMed: 38827321 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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