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 No.: 1884209-98-6
- Formule: C10H17N3O
- Masse moléculaire:195.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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.
Chemical Information
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CAS No. 1884209-98-6
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Masse moléculaire 195.27
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Formule C10H17N3O
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SMILES
N=1C=C(C(=NC1N)OCC(C)(C)C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IACS-4619 Related Classifications
HY-123599 Related Classifications
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