| References: |
DCC-2618 is a small molecule inhibitor of c-Kit and PDGFR with IC50s of 6 nM/30 nM/13 nM for c-Kit/PDGFRα/PDGFRβ respectively.
in vitro: DCC-2618 inhibits normal and mutant KIT kinase at the nanomol level. The targets are wt c-KIT, c-KIT mutants, PDGFR alpha, PDGFR beta, KDR and cFMS. DCC-2618 inhibits mutant KIT in GIST patient cell line (GIST T1 pKIT western Ex11 deletion) at a IC 50 of 2 nM. Deciphera's technology has identified DCC-2618 as a molecule which can be developed as second line therapy for imatinib and sunitinib resistant GIST patients with the potential to progress to frontline GIST therapy. DCC-2618 has been designed to effectively inhibit the imatinib and sunitinib-sensitive KIT juxtamembrane domain mutants (JMD) as well as secondary resistant KIT kinase-domain mutants. DCC-2618 additionally targets PDGFR alpha oncogenic mutants. |
