List of some FLT3 inhibitors. IC50 refers to the concentration required for the inhibition of FLT3 autophosphorylation. “Other receptors” refers to other receptors known to be inhibited by the compound with an IC50 similar to that for FLT3.
Compound . | Chemical Class . | FLT3 IC50 . | Other receptors . | Clinical Trial . |
---|---|---|---|---|
AG1295 | Quinoxaline | 300 nM | PDGFR, KIT | |
AG1296 | Quinoxaline | 300 nM | PDGFR, KIT | |
AGL2043 | Quinoxaline | 100 nM | PDGFR, KIT | |
D64406 | Bis-indlyl- methanone | 300 nM | PDGFR, KIT | |
SU5416 | 3-Substituted indolinone | 100 nM | KIT, VEGFR | Phase I |
SU5614 | 3-Substituted indolinone | 10 nM | KIT, FMS | |
SU11248 | 3-Substituted indolinoneindolinone | 50 nM | KIT, PDGFR, VEGFR | Phase I |
MLN518 | Quinazoline | 30 nM | KIT, PDGFR, | Phase II |
CEP-701 | Indolocarbazole | 2 nM | TRKA | Phase III |
PKC412 | Indolocarbazole | 10 nM | KIT | Phase III planned |
GTP-14564 | Cyclopenta-[a]- inden | 300 nM | KIT, FMS, PDGFR | |
Ki23819 | Quinoline-urea | 1 nM | NR | |
CHIR-258 | Benzimidalzole- quinoline | 10 nM | KIT, FMS, FGFR, VEGFR | Phase 1 |
KW-2449 | NR | 6 nM | FLT3, KIT, Aurora | Phase 1 planned |
Compound . | Chemical Class . | FLT3 IC50 . | Other receptors . | Clinical Trial . |
---|---|---|---|---|
AG1295 | Quinoxaline | 300 nM | PDGFR, KIT | |
AG1296 | Quinoxaline | 300 nM | PDGFR, KIT | |
AGL2043 | Quinoxaline | 100 nM | PDGFR, KIT | |
D64406 | Bis-indlyl- methanone | 300 nM | PDGFR, KIT | |
SU5416 | 3-Substituted indolinone | 100 nM | KIT, VEGFR | Phase I |
SU5614 | 3-Substituted indolinone | 10 nM | KIT, FMS | |
SU11248 | 3-Substituted indolinoneindolinone | 50 nM | KIT, PDGFR, VEGFR | Phase I |
MLN518 | Quinazoline | 30 nM | KIT, PDGFR, | Phase II |
CEP-701 | Indolocarbazole | 2 nM | TRKA | Phase III |
PKC412 | Indolocarbazole | 10 nM | KIT | Phase III planned |
GTP-14564 | Cyclopenta-[a]- inden | 300 nM | KIT, FMS, PDGFR | |
Ki23819 | Quinoline-urea | 1 nM | NR | |
CHIR-258 | Benzimidalzole- quinoline | 10 nM | KIT, FMS, FGFR, VEGFR | Phase 1 |
KW-2449 | NR | 6 nM | FLT3, KIT, Aurora | Phase 1 planned |