5.04972
ATR Inhibitor IV
別名:
ATR Inhibitor IV, VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV
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この商品について
実験式（ヒル表記法）:
C18H16N4O3S
CAS番号:
分子量:
368.41
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
solid
potency
13 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
SMILES string
[S](=O)(=O)(C)c1ccc(cc1)c2nc(c(nc2)N)C(=O)Nc3ccccc3
InChI
1S/C18H16N4O3S/c1-26(24,25)14-9-7-12(8-10-14)15-11-20-17(19)16(22-15)18(23)21-13-5-3-2-4-6-13/h2-11H,1H3,(H2,19,20)(H,21,23)
InChI key
DUIHHZKTCSNTGM-UHFFFAOYSA-N
General description
A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13 nM; IC50/[ATP] = 70 nM/50 µM and 128 nM/100 µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1 µM, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10 µM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120), 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 (≥72 h) in cultures with ATM-p53 pathway defects.Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Other Notes
Prevo, R., et al. 2012, Cancer Biol. Ther.13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol.7, 428.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。