Uses
Fms-like tyrosine kinase (FLT3) is a cell-surface receptor with important roles in stem cell development, hematopoiesis, and cancer. FLT3 Inhibitor is a cell-permeable, ATP-competitive inhibitor of FLT3 (IC50 = 27 nM) that blocks the proliferation of myelomonocytic leukemia MV4-11 cells (IC50 = 0.41 μM). It is selective for FLT3 over a panel of 22 other kinases. FLT3 Inhibitor synergistically increases the cytotoxicity of an AF4-mimetic peptide against MV4-11 cells.
Definition
ChEBI: 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide is a dimethoxybenzene.
Biological Activity
Potent inhibitor of FLT3 receptor tyrosine kinase (IC 50 = 42 nM) that displays selectivity over a range of other kinases. Exhibits antiproliferative effects on MV4-11 cells, a human acute myelogenous leukaemia cell line expressing a constitutively active mutant FLT3 (IC 50 = 340 nM).
References
[1]. trzci′nska-daneluti a.m., nguyen l., jiang c., et al. use of kinase inhibitors to correct δf508-cftr function. molecular & cellular proteomics, 2012, 11(9):745-757.
[2]. patch r.j., baumann c.a., liu j., et al. identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of flt3. bioorganic & medicinal chemistry letters, 2006, 16: 3282-3286.
[3]. kar r.k., suryadevara p., roushan r., et al. quantifying the structural requirements for designing newer flt3 inhibitors. medicinal chemistry, 2012, 8:913-927.
[4]. nishijima c., kawamura k., okamoto n., et al. regulation of preimplantation embryo development in mice by fms-like tyrosine kinase 3 ligand. journal of mammalian ova research, 2014, 31(1):45-51.
[5]. o'farrell a.m., yuen h.a., smolich b., et al. effects of su5416, a small molecule tyrosine kinase receptor inhibitor, on flt3 expression and phosphorylation in patients with refractory acute myeloid leukemia. leuk. res., 2004, 28(7):679-89.
