Gilteritinib (formerly ASP-2215; ASP2215; Trade name: Xospata) is a potent small-molecule inhibitor of FLT3/AXL approved for treating acute myeloid leukemia (AML).
Gilteritinib hemifumarate (ASP2215; ASP-2215 hemifumarate; Xospata), the hemifumarate salt of Gilteritinib (ASP2215), is a marketed anti-AML drug acting as a dual inhibitor of FLT3/AXL with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL respectively.
FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
G-749 (G749) is a novel and potent FLT3 inhibitor with potential antineoplastic activity.
FLT3-IN-4 is a novel,potent and orally effective Fms-like tyrosine receptor kinase 3 inhibitor (FLT3; IC50=7 nM).
UNC-2025 HCl (known also as UNC2025), the Hydrochloride salt of UNC-2025, is an orally bioavailable and selective MER/FLT3 dual inhibitor with potential antineoplastic activity.
Tamatinib besylate (formerly R-406 besylate; prodrug of R 406) is a novel, potent and ATP-competitive inhibitor of spleen tyrosine kinase/Syk with potential anti-inflammatory activity.
Quizartinib HCl (formerly AC220 and AC010220) is a novel, second-generation, and orally bioavailable FLT3 tyrosine kinase inhibitor for Flt3 (ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Quizartinib has displayed potential anticancer activity. AC220 selectively inhibits class III […]
HM-43239 is a novel, selectively and orally active small molecule inhibitor of FLT3.