Preferred Label : BRAFV600/PI3K Inhibitor ASN003;
NCIt definition : A selective inhibitor of mutated forms of B-RAF kinase at amino acid position 600
(BRAFV600), including BRAFV600E, the alpha, delta and, to a lesser extent, beta isoforms
of phosphatidylinositide 3-kinase (PI3K), including mutated forms of PI3KCA, which
encodes the p110-alpha catalytic subunit of the class I PI3K, and the phosphatase
and tensin homologs (PTEN) with loss-of-function mutation, with potential antineoplastic
activity. Upon administration of ASN003, this agent selectively targets, binds to
and inhibits the activity of BRAFV600 mutants as well as mutated isoforms of PI3K.
This inhibits signaling through B-RAF- and PI3K/mechanistic target of rapamycin (mTOR)-mediated
pathways and inhibits cellular proliferation in tumor cells with BRAFV600 mutations,
those expressing PI3K and/or those driven by PTEN. Dysregulation of the B-RAF- and
PI3K-mediated pathways is frequently seen in a variety of tumors and results in increased
tumor cell growth and survival. Dual targeting of both pathways may increase efficacy
and anti-tumor potential compared to the targeting of just one pathway by a selective
B-RAF inhibitor or selective PI3K pathway inhibitor alone.;
Molecule name : ASN 003; ASN-003;
NCI Metathesaurus CUI : CL522477;
Origin ID : C134967;
UMLS CUI : C4525511;
Semantic type(s)
- concept_is_in_subset
- has_target
