1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. FLT3

FLT3

Cluster of differentiation antigen 135; CD135; Fms like tyrosine kinase 3

FLT3 (Fms-like tyrosine kinase 3, CD135) is a protein that in humans is encoded by the FLT3 gene. FLT3 is a cytokine receptor which belongs to the receptor tyrosine kinase class III. FLT3 is the receptor for the cytokine Flt3 ligand (FLT3L). FLT-3 is expressed on the surface of many hematopoietic progenitor cells. Signalling of FLT3 is important for the normal development of haematopoietic stem cells and progenitor cells. The FLT3 gene is one of the most frequently mutated genes in acute myeloid leukemia (AML). Besides, high levels of wild-type FLT3 have been reported for blast cells of some AML patients without FLT3 mutations. These high levels may be associated with worse prognosis. Signaling through FLT3 plays a role in cell survival, proliferation, and differentiation. FLT3 is important for lymphocyte (B cell and T cell) development, but not for the development of other blood cells. Two cytokines that down modulate FLT3 activity are TNF-Alpha and TGF-Beta.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W751180
    3-Hydroxy Midostaurin-13C6
    3-Hydroxy Midostaurin-13C6 (CGP52421-13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412.
    3-Hydroxy Midostaurin-<sup>13</sup>C<sub>6</sub>
  • HY-168114
    Multi-kinase inhibitor 3
    Inhibitor
    Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity.
    Multi-kinase inhibitor 3
  • HY-145904
    PDGFRα/FLT3-ITD-IN-3
    Inhibitor
    PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
    PDGFRα/FLT3-ITD-IN-3
  • HY-144711
    FLT3/ITD-IN-3
    Inhibitor
    FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines.
    FLT3/ITD-IN-3
  • HY-144709
    FLT3/ITD-IN-1
    Inhibitor
    FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines.
    FLT3/ITD-IN-1
  • HY-168982
    Lomonitinib
    Inhibitor
    Lomonitinib is a highly potent and selective pan-FLT3/IRAK4 inhibitor with antitumor activity. Lomonitinib is promising for research of myeloid leukemia.
    Lomonitinib
  • HY-143286
    PF15
    Inhibitor
    PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia.
    PF15
  • HY-155112
    Antiproliferative agent-30
    Inhibitor
    Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation.
    Antiproliferative agent-30
  • HY-123237
    KRC-108
    Inhibitor
    KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice.
    KRC-108
  • HY-161323
    FLT3-ITD/D835Y-IN-1
    Inhibitor
    FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and BCR-ABL inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML).
    FLT3-ITD/D835Y-IN-1
  • HY-158325
    PROTAC FLT-3 degrader 4
    Inhibitor
    PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor).
    PROTAC FLT-3 degrader 4
  • HY-P991208
    Flt-3L-Ig (hum/hum)
    Activator
    Flt-3L-Ig (hum/hum) (hFlt3L) is a Flt3 activator. Flt-3L-Ig (hum/hum) enhances OKT3-induced inflammatory cytokine release from myeloid and dendritic cells in BRGSF-CBC mice, as well as the number and distribution of human immune cells, exhibiting cytokine release syndrome (CRS).
    Flt-3L-Ig (hum/hum)
  • HY-148521
    PROTAC FLT3/CDK9 degrader-1
    Degrader
    PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML.
    PROTAC FLT3/CDK9 degrader-1
  • HY-170689
    CG-3-246
    Inhibitor
    CG-3-246 is a dual inhibitor of FLT3/BCL-2, with the Kds of 63 and 4.25 nM, respectibely. CG-3-246 plays an important role in acute myeloid leukemias research.
    CG-3-246
  • HY-155302
    FLT3-IN-22
    Inhibitor
    FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L.
    FLT3-IN-22
  • HY-170846
    FGFRs-IN-1
    Inhibitor
    FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
    FGFRs-IN-1
  • HY-161280
    PROTAC FLT-3 degrader 3
    Degrader
    PROTAC FLT-3 degrader 3 (compound 35) is a PROTACs degrader of FLT. PROTAC FLT-3 degrader 3 has antiproliferative activity, with IC50 of 7.55 nM in MV4-11 cells.
    PROTAC FLT-3 degrader 3
  • HY-112378
    D-65476
    Inhibitor
    D-65476 is an inhibitor of type Ⅲ receptor tyrosine kinase (Flt3). In the absence of IL-3, D-65476 inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells (IC50= 0.2 μM), which can be used in the study of Flt3-driven leukemia.
    D-65476
  • HY-170576
    FLT3-IN-28
    Inhibitor
    FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD.
    FLT3-IN-28
  • HY-10201S4
    Sorafenib-d3 tosylate
    Inhibitor
    Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-d<sub>3</sub> tosylate
Cat. No. Product Name / Synonyms Species Source