TAK-715

製品コードS2928 バッチS292802

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

C24H21N3OS
分子量 399.51 CAS No. 303162-79-0
Solubility (25°C)* 体外 DMSO 80 mg/mL (200.24 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.
in vitro TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. [1] TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. [2] The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop. [3]
in vivo TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model. [1]

プロトコル(参考用のみ)

キナーゼアッセイ p38 MAP Kinase Assay
Kinase reactions of purified human p38 MAP kinase α are performed at 30 °C for 1 h in kinase reaction buffer (25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol) containing 0.1 μCi [γ-32P]ATP, 500 nM ATP, and myelin basic protein (MBP). The kinase reactions are terminated by the addition of 10% trichloroacetic acid. Phosphorylated proteins are filtrated through GF/C filter plates with a Cell harvester, washing out free [γ-32P]ATP with 250 mM phosphoric acid. The plates are then incubated for 60 min at 45 °C, followed by the addition of 40 μL of MicroScint-O. Radioactivity is counted using a Top-count scintillation counter.
動物実験 動物モデル Adjuvant-induced arthritis (AA) rat model
投薬量 30 mg/kg
投与方法 Orally

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：

Suppression of Lipid Accumulation in the Differentiation of 3T3-L1 Preadipocytes and Human Adipose Stem Cells into Adipocytes by TAK-715, a Specific Inhibitor of p38 MAPK [ Life (Basel), 2023, 13(2)412] PubMed: 36836769
Oleanolic acid induces HCT116 colon cancer cell death through the p38/FOXO3a/Sirt6 pathway [ Chem Biol Interact, 2022, 363:110010] PubMed: 35690101
Inhibition of endothelin-B receptor signaling synergizes with MAPK pathway inhibitors in BRAF mutated melanoma [ Oncogene, 2021, 10.1038/s41388-020-01628-x] PubMed: 33500549
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] PubMed: 31160710
Elucidating essential kinases of endothelin signalling by logic modelling of phosphoproteomics data [ Mol Syst Biol, 2019, 15(8):e8828] PubMed: 31464372
Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [ J Pharmacol Exp Ther, 2019, 370(2):219-230] PubMed: 31189728

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。