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Purity: ≥98%
TCS 359 (TCS-359) is a novel, ATP-competitive and selective fms-like/FLT3 kinase inhibitor with IC50 of 42 nM. TCS 359 inhibited FLT3 ligand's capacity to advance mouse two-cell embryos to the hatched blastocyst stage. In early embryos, TCS 359 also reduced FLT3 ligand expression beyond the four-cell stage. Embryo development was not impacted by TCS 359 in the absence of exogenous FLT3 ligand.
| Targets |
FLT3 (IC50 = 42 nM)
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| ln Vivo |
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| Enzyme Assay |
The isolated kinase domain of the human FLT3 receptor is inhibited using the fluorescence polarization (FP) protocol below in order to assess the compounds of the present invention's activity in an in vitro kinase assay. The Panvera Phospho-Tyrosine Kinase Kit's fluorescein-labeled phosphopeptide and anti-phosphotyrosine antibody are used in the FLT3 fluorescence polarization assay. 30 minutes are spent incubating the FLT3 kinase reaction at room temperature with the following parameters: 10 nM FLT3 571-993, 20μg/mL poly Glu4Tyr, 150μM ATP, 5 mM MgCl2, and 1% compound in DMSO. EDTA is added, and this stops the kinase reaction. After adding the anti-phosphotyrosine antibody and fluorescein-labeled phosphopeptide, the mixture is incubated for 30 minutes at room temperature before the polarization is measured.
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| Cell Assay |
In 100 μL of RPMI media supplemented with 10% FBS, 0.2 ng/mL GM-CSF, penn/strep, and MV4-11 cells, 10,000 cells are plated per well. Cells are cultured for 72 hours under standard cell growth conditions after being treated with compound dilutions or 0.1% DMSO (vehicle control). Each well receives an equal volume of CellTiterGlo reagent, and luminescence is measured to determine total cell growth. The difference between the total number of cells at Day 0 and Day 3 (72 hours of growth and/or compound treatment) in terms of luminescent counts is used to calculate total cell growth. Using non-linear regression analysis and a multiparameter (variable slope) equation, GraphPadPrism is used to calculate all IC50 values.
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| References |
| Molecular Formula |
C18H20N2O4S
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| Molecular Weight |
360.43
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| Exact Mass |
360.11
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| Elemental Analysis |
C, 59.98; H, 5.59; N, 7.77; O, 17.76; S, 8.90
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| CAS # |
301305-73-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
COC1=C(C=C(C=C1)C(=O)NC2=C(C3=C(S2)CCCC3)C(=O)N)OC
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| InChi Key |
FSPQCTGGIANIJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20N2O4S/c1-23-12-8-7-10(9-13(12)24-2)17(22)20-18-15(16(19)21)11-5-3-4-6-14(11)25-18/h7-9H,3-6H2,1-2H3,(H2,19,21)(H,20,22)
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| Chemical Name |
2-[(3,4-dimethoxybenzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.43 mg/mL (3.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7745 mL | 13.8723 mL | 27.7446 mL | |
| 5 mM | 0.5549 mL | 2.7745 mL | 5.5489 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7745 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effect of select kinase inhibitors on ΔF508-CFTR maturation analyzed by immunoblotting. Mol Cell Proteomics. 2012 Sep;11(9):745-57. |
Effect of compounds treatment on the ΔF508-CFTR channel activity in the MDCK cells stably expressing ΔF508-CFTR. Molecular & Cellular Proteomics, 2012, 11(9):745-757. |
Dose response curves of select kinase inhibitors for rescue of ΔF508-CFTR expressed in the MDCK cells. Molecular & Cellular Proteomics, 2012, 11(9):745-757. |
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