IACS-4619
IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target.
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- CAS 番号: 1884209-98-6
- 分子式: C10H17N3O
- 分子量:195.27
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
IACS-4619 shows good MDCK cell permeability, high human plasma protein binding, high liver microsomal turnover, and good plasma stability in rats and humans[1].
IACS-4619 (up to 50 μM) does not confer a robust anti-proliferative phenotype in human cancer cell lines (U2OS, SaOS2, etc.) and normal cell lines (WI38, BJ, etc.)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human cancer cell lines (U2OS, SaOS2, SW480, HCT116, MDAMB231, HeLa, UOK262, 293T, A549, H460, H358) and normal cell lines (WI38, BJ, hMEC, MRC5)
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Concentration:0-50 μM
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Incubation Time:/
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Result:Did not exhibit significant antiproliferative effects or cytotoxicity in any tested cell lines, even with prolonged treatment, and cell lines with high intrinsic ROS levels tolerated the compound well.
化学情報
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CAS 番号 1884209-98-6
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分子量 195.27
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分子式 C10H17N3O
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SMILES
N=1C=C(C(=NC1N)OCC(C)(C)C)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)