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-112475
    Flt-3 Inhibitor III
    		Inhibitor
    Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an 50 of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects.
    Flt-3 Inhibitor III
  • HY-149539
    PLM-101
    		Inhibitor
    PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po).
    PLM-101
  • HY-15163A
    Zotiraciclib hydrochloride
    		Inhibitor
    Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies.
    Zotiraciclib hydrochloride
  • HY-103464
    5'-Fluoroindirubinoxime
    		Inhibitor ≥98.0%
    5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
    5'-Fluoroindirubinoxime
  • HY-139619
    LT-850-166
    		Inhibitor
    LT-850-166 is a potent FLT3 inhibitor with the capacity of overcoming a variety of FLT3 mutations.
    LT-850-166
  • HY-144710
    FLT3/ITD-IN-2
    		Inhibitor
    FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines.
    FLT3/ITD-IN-2
  • HY-15519
    LBW242
    		Inhibitor
    LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells.
    LBW242
  • HY-145690
    HP1328
    		Inhibitor
    HP1328 is a potent inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1328 is a benzoimidazole scaffold-based compound. HP1328 significantly reduces the leukemia burden and prolongs the survival of mice with FLT3/ITD leukemia.
    HP1328
  • HY-143894
    FLT3-IN-11
    		Inhibitor
    FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM).
    FLT3-IN-11
  • HY-155594
    LT-540-717
    		Inhibitor
    LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent.
    LT-540-717
  • HY-112417
    Ki11502
    		Inhibitor 99.30%
    Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.
    Ki11502
  • HY-150582
    c-Met-IN-14
    		Inhibitor
    c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner.
    c-Met-IN-14
  • HY-50905S
    Dovitinib-d8
    		Inhibitor
    Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
    Dovitinib-d<sub>8</sub>
  • HY-168741
    FLT3-ITD-IN-2
    		Inhibitor
    FLT3-ITD-IN-2 (Compound A1) is an inhibitor for FLT3-ITD kinase with an IC50 of 2.12 nM. FLT3-ITD-IN-2 inhibits the proliferation of FLT3-dependent human AML cell line MOLM-13 with an IC50 of 25.65 nM. FLT3-ITD-IN-2 exhibits antitumor efficacy against acute myeloid leukemia.
    FLT3-ITD-IN-2
  • HY-162936
    SILA-123
    		Inhibitor
    SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia.
    SILA-123
  • HY-161709
    FLT3/CDKs ligand-1
    		Degrader
    FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708).
    FLT3/CDKs ligand-1
  • HY-168115
    Multi-kinase inhibitor 4
    		Inhibitor
    Multi-kinase inhibitor 4 (compound 14) is an orally active inhibitor of FLT1, KDR, FLT3, FLT4, PDGFRα, PDGFRβ, with IC50s of 1.97 nM, 1.04 nM, 0.33 nM, 1.44 nM, 0.18 nM, 0.89 nM. Multi-kinase inhibitor 4 plays an important role in cancer research.
    Multi-kinase inhibitor 4
  • HY-157213
    LWY713
    		Degrader
    LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models. LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
    LWY713
  • HY-149474
    HDAC-IN-63
    		Inhibitor
    HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC50: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC50: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML).
    HDAC-IN-63
  • HY-171146
    HSN748
    		Inhibitor
    HSN748 is a Ponatinib (HY-12047) analogue and a multikinase inhibitor. HSN748 has inhibitory activity on FLT3, ABL1, RET, PDGFRα/β, MNK1, MNK2 and other kinases. HSN748 can inhibit the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines and can be used in the study of leukemia.
    HSN748
Cat. No. Product Name / Synonyms Species Source