Quarfloxin (Quarfloxacin; CX-3543) is a novel and potent fluoroquinolone analogue with anticancer activity.

SU14813 is a novel, orally bioavailable, multi-targeted tyrosine kinase inhibitor (TKI) with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT, respectively.

Pexidartinib (formerly PLX-3397; CML-261; FP-113; trade name Turalio) is an orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor of CSF-1R, Kit, and Flt3 with potential antineoplastic activity.

Ripretinib HCl (DCC2618; DCC-2618; Qinlock), the hydrochloride salt of DCC-2618, is an orally bioactive pan KIT and PDGFRA inhibitor approved in 2020 for the treatment of adults with advanced gastrointestinal stromal tumor.

Dasatinib (formerly BMS-354825; trade name Sprycel), an approved anticancer drug, is an orally bioavailable and multi-targeted kinase inhibitorof Abl, Src and c-Kit with potential anticancer activity.

AZD3229 (AZD-3229) is a novel, potent, pan-KIT mutant inhibitor with anticancer activity.

Imatinib Mesylate (also known as STI571 mesylate; trade names: Gleevec or Glivec), the mesylate salt of imatinib, is an orally bioavailable, potent, multi-kinase inhibitor of v-Abl, c-Kit and PDGFR with potential antitumor activity.

Avapritinib (formerly known as BLU-285; trade name Ayvakit) is an oral, potent and selective small molecule inhibitor of PDGFRα D842V and KIT Exon 17 mutants (IC50=0.5 nM) with anticancer activity.

AZD3229 Tosylate, the tosylate salt of AZD-3229, is a novel, potent, pan-KIT mutant inhibitor with antitumor activity.

ISCK03 is a potent c-kit inhibitor.