Preferred Label : Tacaciclib;
NCIt synonyms : Cyclin-dependent Kinase 7 Inhibitor XL102; CDK7 Inhibitor XL102;
NCIt definition : An orally bioavailable, selective inhibitor of cyclin-dependent kinase 7 (CDK7), with
potential antineoplastic activity. Upon oral administration, tacaciclib 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, transcriptional regulation, and promotes the expression of key oncogenes
through the phosphorylation of RNA polymerase II. It's overexpressed in multiple cancers.;
UNII : D3G4JKK1MA;
CAS number : 2768774-66-7;
Molecule name : XL-102; XL 102; AUR102;
NCI Metathesaurus CUI : CL1648441;
Origin ID : C179200;
UMLS CUI : C5555524;
Semantic type(s)
- concept_is_in_subset
- has_target
