VE-821 - Moligand™, 10mM in DMSO , Inhibitor of ATR serine/threonine kinase, CAS No.1232410-49-9, Inhibitor of ATR serine/threonine kinase

CAS: 1232410-49-9 Cat. No.: V408304 Summenformel: C₁₈H₁₆N₄O₃S Molekulargewicht: 368.41 PubChem CID: 51000408

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

VE-821 is a potent and selective ATP competitive inhibitor ofATRwithKi/IC50of 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 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. 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. VE-821 along with cisplatin treatment shows the most marked synergy. VE-821 inhibits H2AX cell growth with IC50 of 800 nM.

In vivo

Cell Data

cell lines：

Concentrations：--

Incubation Time：96 hours

Powder Purity:≥99%

Specifications

Synonyme

2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

VE-821 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.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of ATR serine/threonine kinase

Namen und Kennungen

• Isomere SMILES: CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N
• PubChem CID: 51000408
• Molekulargewicht: 368.41

Zugehörige Ziele (menschlich)

PRKDC Tchem DNA-dependent protein kinase catalytic subunit (1 Activities)

Discover Target: PRKDC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ATR Tchem Serine/threonine-protein kinase ATR (2 Activities)

Discover Target: ATR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 56 mg/mL (201.62 mM); Ethanol: 8 mg/mL (28.8 mM); Water: Insoluble

Referenzen

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] [10.1158/0008-5472.CAN-22-3083]

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1232410-49-9, the molecular formula is C18H16N4O3S, and the molecular weight is 368.41 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.