Preferred Label : Dapolsertib Hydrochloride;
NCIt synonyms : SEL24 Hydrochloride; SEL 24 Hydrochloride; SEL-24 Hydrochloride;
NCIt definition : The hydrochloride salt form of dapolsertib, 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 : 1Z0H0278DB;
CAS number : 2769008-22-0;
NCI Metathesaurus CUI : CL1928928;
Origin ID : C206379;
concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_salt_form_of
