flt-3-in-3

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-38 (Flt-3 Inhibitor II) is a compound that acts as an FLT3 inhibitor. It also exhibits off-target effects by inhibiting the serine/threonine kinase haspin, a mitotic signaling coordinator. FLT3-IN-38 has potential applications in cancer research.

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-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-34 is an FLT3 inhibitor with an IC50 value of 1.4 nM. It inhibits the phosphorylation of FLT3 and downstream signaling molecules AKT and ERK1/2. In FLT3-ITD positive MV4-11 cells, FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis (apoptosis). It exhibits potent antiproliferative activity against FLT3-ITD positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 cells (IC50 = 18.5 nM). FLT3-IN-34 is useful for research on FLT3-positive acute myeloid leukemia (AML).

FLT3-IN-35 (Compound 4K) is an orally active, covalent, irreversible FLT3 inhibitor. It suppresses the phosphorylation of FLT3 and its downstream signaling factors, inducing cell cycle arrest and apoptosis. FLT3-IN-35 has potential applications in the research of acute myeloid leukemia (AML).

FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 nM for FLT3-ITD and 3.4 nM for TEL-VEGFR2. It exhibits high selectivity for FLT3 wild-type (WT) and c-Kit. The compound inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. By causing cell cycle arrest and inducing apoptosis, FLT3-IN-37 demonstrates anti-leukemic activity, making it suitable for research into acute myeloid leukemia (AML).

JAK2/FLT3-IN-3 (11r) is a dual inhibitor of FLT3 and JAK2, with IC50 values respectively at 0.51 nM for FLT3, 2.01 nM for JAK2, and 104.40 nM for JAK3. It can induce apoptosis and exhibits anticancer activity.

LY2457546 is a highly potent, orally bioavailable multi-target anti-angiogenic tyrosine kinase inhibitor. It shows strong inhibitory activity against multiple targets including VEGFR2, PDGFRβ, FLT-3, Tie-2, and Eph family receptors, and is applied in cancer research such as leukemia.

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

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

FLT3 ligand-2 serves as a ligand for the target protein in PROTAC. It is utilized for synthesizing PROTAC FLT-3 degrader 1.

PROTACFLT-3degrader 3 (compound 35) is a PROTAC degrader of FLT. It exhibits antiproliferative activity, with an IC50 value of 7.55 nM in MV4-11 cells.

Flt-3-IN-1 is a potent FLT-3 inhibitor with an IC50 value of 0.91 μM. It induces G1 phase arrest and apoptosis (apoptosis) in leukemia cells. Flt-3-IN-1 is applicable for cancer research, including studies on leukemia.

BPR1J-097) is a novel FLT-3 inhibitor(IC50: 11±7 nM) with promising in vivo anti-tumor activities. It also inhibits FLT-3 D835Y (IC50: 3 nM).

Flt3 Inhibitor IV is a potent ATP-competitive Flt3 inhibitor.

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

Desmorpholinyl Quizartinib-PEG2-COOH is a compound featuring an FLT-3 ligand and a PEG-based PROTAC linker. It is employed in the synthesis of PROTAC FLT-3 degrader 1, which serves as a degrader for the FLT-3 internal tandem duplication (ITD) through PROTAC technology. The degrader exhibits an IC50 of 0.6 nM.

BPR1J-097, a new-type small molecule FLT-3 inhibitor(IC50=11±7 nM), is with great anti-tumor activities in vivo.

Emirodatamab (AMG-427) is an anti-FLT3/CD3 bispecific T-cell engager with an extended half-life. It can induce high cytotoxicity in primary AML progenitor cells and enhance FLT-3 expression. Combining Emirodatamab with anti-PD-1 antibodies increases T-cell dependent cytotoxicity (TDCC). This compound is under investigation for use in relapsed or refractory AML.