217200
ATR Inhibitor IV (VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV)
Size
£581.00
- SKU:
- 217200
- Molecular Weight:
- 368.41
- Storage Conditions:
- -20°C
- Supplier:
- United States Biological
- CAS Number:
- 1232410-49-10
- Extra Details:
- 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 4°C. For long-term storage store at -20°C. 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.
- Shipping Conditions:
- Blue Ice