Home Angiogenesis FLT3 inhibitor TCS 359 For research use only.

TCS 359

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

TCS 359 Chemical Structure

TCS 359 Chemical Structure

CAS: 301305-73-7

Selleck's TCS 359 has been cited by 2 publications

Purity & Quality Control

Batch: S802301 DMSO] 15 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.89%
99.89

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Signaling Pathway

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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
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]
Kinase Assay 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 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.

Chemical Information & Solubility

Molecular Weight 360.43 Formula

C18H20N2O4S
CAS No. 301305-73-7 SDF Download TCS 359 SDF
Smiles COC1=C(C=C(C=C1)C(=O)NC2=C(C3=C(S2)CCCC3)C(=O)N)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 15 mg/mL ( (41.61 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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