Description:
IC50 Value: 6 nM and 9 nM for wt c-KIT and KIT V654A exon 13 respectively; 30 nM and 13 nM for PDGFR alpha and beta respectively [1].
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 [1]. 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.
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 [1].
in vivo: N/A
Clinical trial: N/A