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

FLT3

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

FLT3

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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-115443
    MZH29
    		Inhibitor
    MZH29 is a potent and orally active FLT3 inhibitor. MZH29 shows inhibitory effects on wild-type and mutant FLT3, including the FLT3-ITD, FLT3-D835H/Y/V and FLT3-K663Q mutants. MZH29 retains its potent inhibitory effect against the FLT3-ITD/F691L mutation, a drug resistance mutation against the well-known FLT3 inhibitor, AC220 (HY-13001). MZH29 can be used for the research of cancer, such as acute myeloid leukemia (AML).
    MZH29
  • 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-16449
    SB1578
    		Inhibitor
    SB1578 (CT-1578) is a selective JAK2 and FLT3 inhibitor with an IC50 of 46 nM and 60 nM, respectively. SB1578 exhibits high selectivity for other kinase targets. SB1578 can be used for the study of non-oncology indication rheumatoid arthritis.
    SB1578
  • 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-E70724
    FLT3 ITD Recombinant Human Active Protein Kinase
    FLT3 (FMS-like tyrosine kinase 3, CD135) is a type 3 receptor tyrosine kinase that plays important roles in cell survival, proliferation, and differentiation during normal hematopoiesis. FLT3 is one of the most frequently mutated genes in acute myeloid leukemia (AML). FLT3 ITD is a internal tandem duplication (ITD) mutation of FLT3 that may be present in AML cells. FLT3 ITD Recombinant Human Active Protein Kinase is a recombinant FLT3 ITD protein that can be used to study FLT3 ITD-related functions.
    FLT3 ITD Recombinant Human Active Protein Kinase
  • 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-178444
    Flt-3-IN-1
    		Inhibitor
    Flt-3-IN-1 is a potent FLT-3 inhibitor with an IC50 of 0.91 μM. Flt-3-IN-1 can cause leukemia cells G1 phase arrest and induce apoptosis. Flt-3-IN-1 can be used for the research of cancer, such as leukemia.
    Flt-3-IN-1
  • HY-175473
    HI042
    		Inhibitor
    HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML).
    HI042
  • 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-123586
    L-783277
    		Inhibitor
    L-783277 (Compound 4) is a MEK inhibitor (IC50 = 4 nM). L-783277 has potent inhibitory activity against a variety of kinases, including VEGFR2/3, FLT1/3/4, MEK1/2, KDR, and PDGFRα, but has low selectivity for the kinase community. L-783277 inhibits viability (IC50 = 22 mM) and cell proliferation (IC50 = 21 mM) of H295R cells. L-783277 could be used in research on cancers such as adrenocortical carcinoma.
    L-783277
  • 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
Cat. No. Product Name / Synonyms Species Source