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| | TCS 359 Basic information |
| Product Name: | TCS 359 | | Synonyms: | 2-(3,4-DIMETHOXY-BENZOYLAMINO)-4,5,6,7-T;TCS359;2-(3,4-Dimethoxy-benzoylamino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid amide;Flt-3 inhibitor;2-[(3,4-Dimethoxybenzoyl)amino]-4,5,6,7-benzo[b]thiophene-3-carboxamide;2-(3,4-diMethoxybenzaMido)- 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxaMide;Benzo[b]thiophene-3-carboxaMide,2-[(3,4-diMethoxybenzoyl)aMino]-4,5,6,7-tetrahydro-;2-[(3,4-Dimethoxybenzoyl)amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxamide | | CAS: | 301305-73-7 | | MF: | C18H20N2O4S | | MW: | 360.43 | | EINECS: | | | Product Categories: | API;Inhibitors | | Mol File: | 301305-73-7.mol |  |
| | TCS 359 Chemical Properties |
| Boiling point | 454.4±45.0 °C(Predicted) | | density | 1.328±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Sealed in dry,Store in freezer, under -20°C | | solubility | H2O: <2mg/mL | | pka | 12.43±0.20(Predicted) | | form | White solid | | color | white to off-white | | Sensitive | Light Sensitive | | CAS DataBase Reference | 301305-73-7 |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 | | HS Code | 2934.99.4400 |
| | TCS 359 Usage And Synthesis |
| 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. | | Uses | TCS 359 is a potent inhibitor of FLT3 used in the treatment of leukemia. | | 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). | | storage | Store at +4°C | | 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. |
| | TCS 359 Preparation Products And Raw materials |
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