Home Angiogenesis FLT3 inhibitor TCS 359

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TCS 359 FLT3 inhibitor

Cat.No.S8023

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

Chemical Structure

Molecular Weight: 360.43

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 15 mg/mL (41.61 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 360.43 Formula

C18H20N2O4S

 Storage (From the date of receipt)
CAS No. 301305-73-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C(C=C1)C(=O)NC2=C(C3=C(S2)CCCC3)C(=O)N)OC

Mechanism of Action

Features
Highly potent and selective.
Targets/IC50/Ki
FLT3
42 nM
In vitro
TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent inhibitor of FLT3 with IC50 of 42 nM. This compound inhibits MV4-11 proliferation with IC50 of 340 nM. It is highly selective for FLT3 against a panel of kinases.
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% this 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.
References

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