VE-821

製品コードS8007 バッチS800703

印刷

化学情報

Synonyms

ATR inhibitor IV

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₆N₄O₃S

分子量

368.41

CAS No.

1232410-49-9

Solubility (25°C)*

体外

DMSO

74 mg/mL (200.86 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with K_i/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.
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 (K_is of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. This compound 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] This chemical inhibits H2AX cell growth with IC50 of 800 nM. ^[2]
in vivo	VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR.

製品説明

VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with K_i/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.

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 (K_is of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. This compound 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]

This chemical inhibits H2AX cell growth with IC50 of 800 nM. ^[2]

in vivo

VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR.

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase inhibition
キナーゼアッセイ	The ability of compounds to inhibit ATR, ATM or DNAPK kinase activity is tested using a radiometric-phosphate incorporation assay. A stock solution is prepared consisting of the appropriate buffer, kinase, and target peptide. To this is added the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [γ-³³P]ATP solution and incubated at 25 ℃. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared as per manufacturer
細胞アッセイ	細胞株	H2AX cells
	濃度	--
	反応時間	96 hours
	実験の流れ	Cells are plated in 96-well plates and allowed to adhere overnight. The following day, this compound is added at the indicated concentrations in a final volume of 200μL, and the cells are then incubated for 96 h. MTS reagent (40μL) is then added, and 1 h later, absorbance at 490 nm is measured using a SpectraMax Plus 384 plate reader. Synergy and antagonism are assessed using Macsynergy software.
動物実験	動物モデル	Male immunodefcient mice
	投薬量	15 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/21490603/
http://www.ncbi.nlm.nih.gov/pubmed/?term=21413798
https://pubmed.ncbi.nlm.nih.gov/34998399/

カスタマーフィードバック

: 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

DNA2 enables growth by restricting recombination-restarted replication [ Nature, 2025, 646(8086):992-1000]	PubMed: 40903580
KEAP1 and STK11/LKB1 alterations enhance vulnerability to ATR inhibition in KRAS mutant non-small cell lung cancer [ Cancer Cell, 2025, 43(8):1530-1548.e9]	PubMed: 40645185
Insufficient telomeric DNA damage response promotes chromosomal instability in aged oocytes [ Sci Bull (Beijing), 2025, S2095-9273(25)00865-5]	PubMed: 40930920
The DNA replication machinery transmits dual signals to prevent unscheduled licensing and execution of centrosome duplication [ Nat Commun, 2025, 16(1):7799]	PubMed: 40921755
The DNA replication checkpoint prevents PCNA/RFC depletion to protect forks from HLTF-induced collapse in human cells [ Mol Cell, 2025, 85(13):2474-2486.e6]	PubMed: 40578346
Inhibition of DEK restores hematopoietic stem cell function in Fanconi anemia [ J Exp Med, 2025, 222(3)e20241248]	PubMed: 39836085
Autophosphorylation of the Tousled-like kinases TLK1 and TLK2 regulates recruitment to damaged chromatin via PCNA interaction [ Nucleic Acids Res, 2025, 53(4)gkae1279]	PubMed: 39727191
Nuclear rupture in confined cell migration triggers nuclear actin polymerization to limit chromatin leakage [ EMBO J, 2025, 44(21):6112-6136]	PubMed: 40983686
REV7 functions with REV3 as a checkpoint protein delaying mitotic entry until DNA replication is completed [ Cell Rep, 2025, 44(4):115431]	PubMed: 40106439
DSCC1 restrains 53BP1/RIF1 signaling at DNA double-strand breaks to promote homologous recombination repair [ Cell Rep, 2025, 44(4):115452]	PubMed: 40117291

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。