ATR Inhibitor IV (VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV), CAS [[1232410-49-10]]

Produktübersicht

• Artikelname: ATR Inhibitor IV (VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV), CAS [[1232410-49-10]]
• Artikelnummer: USB-217200
• Hersteller Artikelnummer: 217200
• Alternativnummer: USB-217200-10
• Hersteller: US Biological
• Kategorie: Biochemikalien

Produktbeschreibung

A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13nM, IC50/[ATP] = 70nM/50uM and 128nM/100uM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1uM, respectively, against DNA-PK, PI 3-K-gamma, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10uM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24h) VE-821 treatment, either alone or in synergy with Cisplatin, results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (72h) in cultures with ATM-p53 pathway defects. Synonyms: VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV CAS No: 1232410-49-10 Molecular Formula: C18H16N4O3S Solubility: As Reported Primary Target: ATR Primary Target Ki: 13nM Molar Mass: 368.41 Appearance: Yellow solid Purity: 98% (HPLC) Storage and Stability: May be stored at 4C. For long-term storage store at -20C. Stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Store under inert gas. Light sensitive.

Produkteigenschaften

• Molekulargewicht: 368.41
• Reinheit: 98% (HPLC)
• Formulierung: Yellow solid
• CAS Nummer: [1232410-49-10]