MAX-40279 hemifumarate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032).

MAX-40279 hemiadipate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032).

OTS447 is a potent FLT3 inhibitor with an IC50 of 21 nM (WO2012016082A1, compound 335).

FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM).

K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase.

FF-10101 (FF10101) is a potent, selective, and irreversible FLT3 inhibitor with IC50 of 0.14 nM (FLT3 Wt), covalent binds to the C695 residue of FLT3.FF-10101 potently inhibited the phosphorylation of FLT3-ITD than that of FLT3-ITD-C695S (IC50 values 2.4 nM and 79 nM, respectively).FF-10101 potently and selectively inhibits the growth of mutant FLT3-expressing leukemia cells in vitro (MV4-11 c ell, IC50=0.83 nM), potently inhibits kinase activities of wild-type FLT3 and FLT3-D835Y with IC50 values of 0.20 nM and 0.16 nM, respectively.FF-10101 demonstrated high kinase selectivity to wild-type FLT3 with >30-fold margins against the other kinases except for FMS and KIT with IC50 values of 0.94 nM and 2.0 nM, respectively.FF-10101 showed growth inhibitory effects on all tested types of FLT3-TKD mutation- and FLT3-ITD with D835Y, Y842C, Y842H, or F691L mutation-expressing 32D cells with GI50 values from 0.43 nM to 6.1 nM.FF-10101 (2, 5, and 10 mg/kg) demonstrated anti-leukemic effects in in vivo models, FF-10101 more potently inhibited the growth of tumors with FLT3-ITD-D835Y and FLT3-ITD-F691L than quizartinib.

Danatinib is a potent and selective FLT3 inhibitor with IC50 of 3 nM, overcomes acquired resistance and shows effective inhibition against FLT3-ITD and/or FLT3-TKD mutations.

MBP-11901 is an orally active, multitarget tyrosine kinase inhibitor targeting FLT3, VEGFR2, PDGFRβ, and c-KIT, shows excellent inhibitory activity against HCC cell growth in vitro (HepG2, IC50=5.16 uM).

PCW-A1001 is a potent, selective inhibitor of FLT-3 (D835Y) mutant with IC50 of 764 nM, weakly inhibits WT FLT-3 with IC50 of 2.54 uM.

TSN084 (TSN 084) is a unique small molecule multi-kinase inhibitor of drug-resistant mutations of c-Met, Trks, and Flt3, also inhibits other oncotargets including Axl, DDRs, and CDK8/19.

YHJ1039 is a broad-spectrum kinase inhibitor, possesses excellent potencies against FLT3 mutants (FLT3 D835Y, IC50=0.41 nM) as well as FAK (IC50=7 nM).