Description
Key facts
CAS number:301305-73-7,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:360.4 Da,
Molecular formula:C18H20N2O4S,
PubChem:1048845,
Nature:Synthetic,
Solubility:Soluble in DMSO to 25 mM,
Biochemical name:Flt-3 inhibitor,
Biological description:Potent FLT3 receptor tyrosine kinase inhibitor (IC50 = 42 nM). Selective over 22 other kinases. Shows antiproliferative effects (IC50 = 340 nM for Human acute myelocytic leukemia MV4-11 cells).,
Canonical smiles:COC1=C(C=C(C=C1)C(=O)NC2=C(C3=C(S2)CCCC3)C(=O)N)OC,
InChi:InChI=1S/C18H20N2O4S/c1-23-12-8-7-10(9-13(12)24-2)17(22)20-18-15(16(19)21)11-5-3-4-6-14(11)25-18/h7-9H,3-6H2,1-2H3,(H2,19,21)(H,20,22),
InChiKey:FSPQCTGGIANIJZ-UHFFFAOYSA-N,
IUPAC Name:2-[(3,4-dimethoxybenzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-+4°C, Appropriate long-term storage conditions-+4°C, Storage information-The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Flt3 also known as CD135 or FLT3 tyrosine kinase is a receptor tyrosine kinase that belongs to the class III receptor tyrosine kinase family. It has a molecular weight of approximately 160 kDa. This protein plays an important role in the development of hematopoietic stem and progenitor cells. Flt3 is expressed mainly in early progenitor cells within the bone marrow. Additionally it is present in some populations of mature cells in the peripheral blood and lymphoid organs.
Biological function summary
Flt3 functions as a receptor that is activated by binding to its ligand FLT3 ligand (FLT3L). This interaction stimulates the associated tyrosine kinase activity leading to auto-phosphorylation of Flt3 and subsequent downstream signaling. Flt3 does not form a heterocomplex rather it dimerizes upon ligand binding to initiate signaling cascades. These cascades promote cell proliferation differentiation and survival particularly impacting hematopoiesis and immune responses.
Pathways
Flt3 signaling impacts the internal signaling networks involving the MAPK/ERK and PI3K/AKT pathways both central to cell cycle regulation and apoptosis. Flt3 interacts functionally with proteins such as SHP2 and GRB2 in these pathways aiding signal transduction. The Flt3 receptor also shares functional motifs with KIT and PDGF receptors indicating shared regulatory mechanisms involved in cellular proliferation.
Flt3 mutations especially internal tandem duplications in Flt3/ITD are significant in acute myeloid leukemia (AML) leading to abnormal cell growth and survival. These mutations often co-occur with other genetic anomalies such as NPM1 mutations contributing to the oncogenic process. The abnormal activation of Flt3 kinase activity also has ramifications in myelodysplastic syndromes making it a target for therapeutic intervention with drugs such as anti-FLT3 inhibitors in the treatment regime.
