Preferred Label : Mocaciclib;
NCIt synonyms : Cyclin-dependent Kinase 7 Inhibitor Q901; CDK7 Inhibitor Q901;
NCIt definition : A selective inhibitor of cyclin-dependent kinase 7 (CDK7), with potential antineoplastic
activity. Upon administration, mocaciclib selectively targets, covalently binds to
and inhibits the activity of CDK7, thereby inhibiting CDK7-mediated signaling. The
inhibition of CDK7 prevents phosphorylation of the carboxy-terminal domain (CTD) of
RNA polymerase II, thereby preventing transcription of important cancer-promoting
genes. It prevents phosphorylation of the cell cycle kinases CDK1, 2, 4, and 6, thereby
disrupting uncontrolled cell cycle progression. Altogether, this may induce apoptosis,
cause cell cycle arrest, inhibit DNA damage repair and inhibit tumor cell proliferation
in certain cancers that are dependent on CDK7-mediated transcriptional regulation
and signaling. CDK7, a serine/threonine kinase, plays a role in controlling cell cycle
progression and transcriptional regulation, and promotes the expression of key oncogenes
through the phosphorylation of RNA polymerase II. It is overexpressed in multiple
cancers.;
UNII : PZU3J2EH9A;
CAS number : 2766124-39-2;
Molecule name : Q-901; Q 901; CDK7-IN-21;
NCI Metathesaurus CUI : CL1792747;
Origin ID : C211797;
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