Preferred Label : Emidurdar;
NCIt synonyms : Endovion; N-(4-bromo-2-(1h-1,2,3,4-tetrazol-5-yl)phenyl)-N'-(3,5-bis(trifluoromethyl)phenyl)urea; SRPK1/ABCG2 Inhibitor SCO-101; Urea, N-(3,5-bis(trifluoromethyl)phenyl)-N'-(4-bromo-2-(1H-tetrazol-5-yl)phenyl)-;
NCIt definition : An orally bioavailable inhibitor of the serine/arginine-rich splicing factor protein
kinase 1 (SRPK1) and the ATP-binding cassette sub-family G member 2 (ABCG2), with
potential chemosensitizing and antineoplastic activities. Upon oral administration,
emidurdar targets, binds to and inhibits the activity of SRPK1 and ABCG2. Inhibition
of the cellular efflux pump ABCG2 by emidurdar prevents the efflux of co-administered
chemotherapeutic agents from cancer cells. This may abrogate cancer cell drug resistance
and may re-sensitize cancer cells to the chemotherapeutic agents. Inhibition of SRPK1
kinase by emidurdar inhibits the SRPK1-mediated phosphorylation of splicing factors
rich in serine/arginine domains, thereby inhibiting the activation of proteins that
are involved in the regulation of alternative splicing. This may inhibit cancer cell
proliferation. SRPK1 is upregulated in various cancer cell types. Its upregulation
is correlated with higher tumor staging, grading, and shorter survival.;
UNII : 943YH53W21;
CAS number : 265646-85-3;
Molecule name : SCO 101; SCO-101; NS 3728; NS-3728;
NCI Metathesaurus CUI : CL1412867;
Origin ID : C175512;
UMLS CUI : C5446585;
Semantic type(s)
- concept_is_in_subset
