Preferred Label : Dapolsertib;
NCIt synonyms : Dual PIM/FLT3 Kinase Inhibitor; PIM/FLT3 Kinase Inhibitor SEL24;
NCIt definition : An orally available inhibitor of PIM family serine/threonine protein kinases and mutant
forms of FMS-related tyrosine kinase 3 (FLT3; STK1) with potential antineoplastic
activity. Upon oral administration, dapolsertib binds to and inhibits the kinase activities
of PIM-1, -2 and -3, and mutant forms of FLT3, which may result in the interruption
of the G1/S phase cell cycle transition, an inhibition of cell proliferation, and
an induction of apoptosis in tumor cells that overexpress PIMs or express mutant forms
of FLT3. FLT3, a tyrosine kinase receptor that is overexpressed or mutated in various
cancers, plays a role in signaling pathways that regulate hematopoietic progenitor
cell proliferation, and in leukemic cell proliferation and survival. PIM kinases,
downstream effectors of many cytokine and growth factor signaling pathways, including
the FLT3 signaling pathway, play key roles in cell cycle progression and apoptosis
inhibition and may be overexpressed in various malignancies.;
UNII : 9M7X64VTLI;
CAS number : 1616359-00-2;
Molecule name : SEL24-B489; SEL 24; SEL24;
NCI Metathesaurus CUI : CL520500;
Origin ID : C133540;
UMLS CUI : C4524702;
Semantic type(s)
- concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
