Preferred Label : Luxeptinib;
NCIt synonyms : Pan-FLT3/Pan-BTK Inhibitor CG-806; Pan-FLT3/BTK Multi-Kinase Inhibitor CG 806; FLT3/BTK Inhibitor CG 806; Pan-FLT3/Pan-BTK Multi-kinase Inhibitor CG-806; 32,72,74,76-Tetrafluoro-14-methyl-21,23-dihydro-11h-4,6-diaza-2(4,7)-isoindola- 1(2)-imidazola-3(1,4),7(1)-dibenzenaheptaphane-2,35-dione;
NCIt definition : An orally bioavailable reversible, pan-inhibitor of both FMS-like tyrosine kinase
3 (FLT3; CD135; STK1; FLK2) and Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia
tyrosine kinase), with potential antineoplastic activity. Upon oral administration,
luxeptinib targets, non-covalently binds to and inhibits the activity of both FLT3,
including both wild-type (WT) FLT3 and FLT3-ITD (internal tandem duplications), tyrosine
kinase domain (FLT3-TKD), and gatekeeper (FLT3-F691L) mutant forms, and BTK, including
both the WT and its C481S mutant (BTK-C481S) form. This inhibits both uncontrolled
FLT3-mediated and B-cell antigen receptor (BCR)-mediated signaling, respectively.
This results in the inhibition of proliferation in tumor cells overexpressing FLT3
and BTK. In addition, CG-806 also inhibits, to a lesser degree, other oncogenic kinases,
such as MET, RET, discoidin domain-containing receptor 2 (DDR2), Aurora kinase A,
and interleukin-2-inducible T-cell kinase (ITK). FLT3, a class III receptor tyrosine
kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute
myeloid leukemias (AMLs), and plays a key role in tumor cell proliferation. BTK, a
member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases essential
to BCR signaling, is overexpressed or mutated in B-cell malignancies; it plays an
important role in the development, activation, signaling, proliferation and survival
of B-lymphocytes.;
UNII : TQ6PBX1JU0;
CAS number : 1616428-23-9; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1616428-23-9
alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo
G-SRS /a ;
Molecule name : CG 806; CG-806; CG-026806;
NCI Metathesaurus CUI : CL971079;
Origin ID : C162573;
UMLS CUI : C5554565;
Semantic type(s)
- concept_is_in_subset
- has_target
