1627696-51-8C[C@@]1(c2ncncc2F)NC(=O)c2cc(-c3cn[nH]c3)ccc21KNLVLWZENYQYRT-MRXNPFEDSA-NCDC7 Kinase Inhibitor LY3143921 is an orally bioavailable inhibitor of cell division cycle 7 (CDC7) kinase, with potential antineoplastic activity. Upon administration, CDC7 kinase inhibitor LY3143921 targets, binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. The serine-threonine kinase CDC7 plays a key role in DNA replication by binding to and phosphorylating serine (Ser)-40 and 53 of MCM2 (minichromosome maintenance complex component 2), which is required for the initiation of DNA replication. Although expressed at low levels in healthy, normal cells, CDC7 is expressed at much higher levels in cancer cells.
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BeschreibungLY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay). It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 μM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.
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CHEMBL6068779