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 No. 301305-73-7

Purity & Quality Control

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

TCS 359 Related Products

Signaling Pathway

FLT3 Signaling Pathways

FLT3 Signaling Pathway

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy TCS 359 | TCS 359 supplier | purchase TCS 359 | TCS 359 cost | TCS 359 manufacturer | order TCS 359 | TCS 359 distributor