TCS 359

Catalog No.S8023

TCS 359 Chemical Structure

Molecular Weight(MW): 360.43

TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
USD 470 In stock
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Biological Activity

Description TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.
Features Highly potent and selective.
Targets
FLT3 [1]
42 nM
In vitro

TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent inhibitor of FLT3 with IC50 of 42 nM. TCS 359 inhibits MV4-11 proliferation with IC50 of 340 nM. TCS 359 is highly selective for FLT3 against a panel of kinases. [1]

Protocol

Kinase Assay:[1]
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Affinity determination:

To determine the activity of the compounds of the present invention in an in vitro kinase assay, inhibition of the isolated kinase domain of the human FLT3 receptor is performed using the following fluorescence polarization (FP) protocol. The FLT3 fluorescence polarization assay utilizes the fluorescein-labeled phosphopeptide and the anti-phosphotyrosine antibody included in the Panvera Phospho-Tyrosine Kinase Kit. The FLT3 kinase reaction is incubated at room temperature for 30 min under the following conditions: 10 nM FLT3 571-993, 20μg/mL poly Glu4Tyr, 150μM ATP, 5 mM MgCl2, and 1% compound in DMSO. The kinase reaction is stopped with the addition of EDTA. The fluorescein-labeled phosphopeptide and the anti-phosphotyrosine antibody are added and incubated for 30 min at room temperature and polarization is read.
Cell Research:[1]
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  • Cell lines: MV4-11
  • Concentrations: ~5 μM
  • Incubation Time: 72 hours
  • Method: MV4-11 cells are plated at 10,000 cells per well in 100 μL of in RPMI media containing penn/strep, 10% FBS, and 0.2 ng/mL GM-CSF. Compound dilutions or 0.1% DMSO (vehicle control) is added to cells and the cells are allowed to grow for 72 h at standard cell growth conditions. To measure total cell growth, an equal volume of CellTiterGlo reagent is added to each well and luminescence is quantified. Total cell growth is quantified as the difference in luminescent counts of cell number at Day 0 compared to total cell number at Day 3 (72 h of growth and/or compound treatment). All IC50 values are calculated in GraphPadPrism using non-linear regression analysis with a multiparameter (variable slope) equation.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (41.61 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 360.43
Formula

C18H20N2O4S

CAS No. 301305-73-7
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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FLT3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID