FLT

FLT3-IN-3 is an effective FLT3 inhibitor, and the IC50s of FLT3 WT and FLT3 D835Y are 13 and 8 nM, respectively.

FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD [FLT3 mutation], with an IC50 of 1.336 nM.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.

FLT3-IN-2 is an FLT3 inhibitor (IC50<1 μM).

TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.

Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively).

CHMFL-FLT3-122 is a potent and orally available FLT3 kinase inhibitor used to treat FLT3-ITD positive acute myeloid leukemia. CHMFL-FLT3-122 significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft model (50 mg/kg) without exhibiting obvious toxicity in vivo.

FLT3-IN-16 exhibits potent inhibitory activity against FLT3 tyrosine kinase with an IC 50 of 1.1 μM. FLT3-IN-16 can be used for researching acute myeloid leukemia [1].

FLT3-IN-10 (2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-) (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 shows the potential for the treatment of FLT3-mutated acute myeloid leukemia (AML).

FLT3-IN-32 hydrochloride is a potent, orally active FLT3 inhibitor with IC50 values of 0.29 nM for FLT3-ITD, 0.77 nM for FLT3-D835Y, and 2.07 nM for FLT3-N676K. It induces apoptosis in FLT3-mutant Ba/F3 cells by reducing the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT). In MV4-11 xenograft models, it demonstrates significant antitumor effects. This compound is suitable for research in acute myeloid leukemia (AML).

FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM for FLT3 and 0.199 nM for the FLT3/D835Y mutant. It demonstrates significant antiproliferative effects against MV4-11 cells and Ba/F3 cell lines expressing mutant FLT kinase variants, including FLT-D835Y and FLT3-F691L [1].

FLT3-IN-4 (FLT3 inhibitor 9u) is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor ,for treating acute myelogenous leukemia.

FLT3-ITD-IN-2 (Compound A1) is an inhibitor of the FLT3-ITD kinase, exhibiting an IC50 of 2.12 nM. It effectively suppresses the proliferation of the FLT3-dependent human AML cell line MOLM-13, with an IC50 of 25.65 nM. FLT3-ITD-IN-2 demonstrates antitumor activity against acute myeloid leukemia.

FLT3-IN-32 is a potent FLT3 inhibitor with high selectivity, effectively suppressing FLT3 activating mutations and inducing apoptosis. It demonstrates good tolerance in non-tumor-bearing mice. In NOD/SCID mice loaded with MV4-11 cells, FLT3-IN-32 exhibits outstanding antitumor efficacy, significantly extending mouse survival. FLT3-IN-32 is applicable for acute myeloid leukemia research.

FLT3-IN-31 (compound 10q) is a potent FLT3 inhibitor, with IC50 values of 0.16 nM for FLT3 and 2.4 nM for FLT3-D835Y, exhibiting antiproliferative activity. It reduces protein expression of p-FLT3, P-STAT5, and P-ERK. Additionally, FLT3-IN-31 induces apoptosis and causes cell cycle arrest at the G1 phase, displaying antitumor properties.

FLT3-IN-33 (Compound 7r) is a potent FLT3 inhibitor with an IC50 of 7.82 nM. It exhibits excellent anticancer activity against acute myeloid leukemia (AML) cells, such as MV4-11 and MOLM-13 cells. FLT3-IN-33 significantly induces apoptosis and inhibits the phosphorylation of the FLT3 pathway, making it useful for research in AML and other cancers.

FLT3-IN-32 TFA is a potent FLT3 inhibitor with IC50 values of 2.40 nM and 3.83 nM against FLT3-ITD and FLT3-D835Y, respectively. It effectively inhibits the proliferation/survival of human MV4-11 cells with an IC50 of 0.07 nM. FLT3-IN-32 TFA is applicable in acute myeloid leukemia (AML) research.

FLT3-IN-13 (compound 20) is a highly effective inhibitor targeting both topoisomerase II and FLT3 proteins in leukemic cells, with IC50 values of 2.26 μM for both. It induces cell cycle arrest at the G2/M phase, promotes apoptosis, and displays considerable anticytotoxic activity specifically against leukemia [1].

FLT3/ITD-IN-1 (Compound 1) is a highly potent inhibitor of FLT3 internal tandem duplications (FLT3-ITD) with IC50 values of 38.2 nM for FLT3 and 144.1 nM for FLT3-ITD, and shows exceptional antiproliferative activities against several acute myeloid leukemia cell lines [1].

FLT3/D835Y-IN-1 (compound 13a) is an orally active, selective inhibitor of FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively. It exhibits anticancer efficacy and has research value in AML (acute myeloid leukemia).

FLT3-IN-11 (compound 30) is an orally active, potent, and selective inhibitor of FLT3 kinase that targets wild-type FLT3 (IC50: 7.22 nM) and FLT3-D835Y (IC50: 4.95 nM), demonstrating significant anti-AML effects with an IC50 value of 3.2 nM for MV4-11 cells.

FLT3-IN-12 is a selective, potent, orally active FLT3 kinase inhibitor that acts on FLT3-WT (IC50: 1.48 nM) and FLT3-D835Y (IC50: 2.87 nM). FLT3-IN-12 is more selective than c-KIT (>1000-fold). FLT3-IN-12 showed significant anti-AML effects, with an IC50 value of 0.75 nM for MV4-11 cells.

FLT3-IN-15 is an orally active and potent FLT3 inhibitor, capable of acting on FLT3 (IC50: 0.87 nM) and FLT3/D835Y (IC50: 0.32 nM).

FLT3/TrKA-IN-1 is a potent dual kinase inhibitor that targets FLT3 (IC50: 43.8 nM), FLT3-ITD (IC50: 97.2 nM), FLT3-TKD (IC50: 92.5 nM), and TrKA (IC50: 23.6 nM). FLT3/TrKA-IN-1 shows potential for acute myeloid leukaemia (AML) studies.