301305-73-7 Usage
Description
TCS 359 is a cell-permeable, ATP-competitive inhibitor of Fms-like tyrosine kinase (FLT3), a cell-surface receptor that plays a crucial role in stem cell development, hematopoiesis, and cancer. It selectively targets FLT3 over a panel of 22 other kinases, making it a promising pharmaceutical candidate for the treatment of leukemia.
Uses
Used in Oncology:
TCS 359 is used as a potent FLT3 inhibitor for the treatment of leukemia. It effectively blocks the proliferation of myelomonocytic leukemia MV4-11 cells, demonstrating an IC50 of 0.41 μM. Additionally, TCS 359 synergistically increases the cytotoxicity of an AF4-mimetic peptide against MV4-11 cells, enhancing its therapeutic efficacy in the treatment of leukemia.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 301305-73-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,0,1,3,0 and 5 respectively; the second part has 2 digits, 7 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 301305-73:
(8*3)+(7*0)+(6*1)+(5*3)+(4*0)+(3*5)+(2*7)+(1*3)=77
77 % 10 = 7
So 301305-73-7 is a valid CAS Registry Number.
InChI:InChI=1/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)