TCS 359

製品コードS8023 バッチS802301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H20N2O4S
分子量 360.43 CAS No. 301305-73-7
Solubility (25°C)* 体外 DMSO 15 mg/mL (41.61 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 TCS 359 is a potent FLT3 inhibitor with IC50 of 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]
特徴 Highly potent and selective.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 MV4-11
濃度 ~5 μM
反応時間 72 hours
実験の流れ 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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Inositol treatment inhibits medulloblastoma through suppression of epigenetic-driven metabolic adaptation [ Nat Commun, 2021, 12(1):2148] PubMed: 33846320
Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6. [ Blood, 2016, 127(23):2890-90] PubMed: 27099147

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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