2-(メチルスルフィニル)-4-メチル-6-(3-アミノベンジル)-4H-チエノ[2′,3′:4,5]ピロロ[2,3-d]ピリダジン-5(6H)-オン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

2-(メチルスルフィニル)-4-メチル-6-(3-アミノベンジル)-4H-チエノ[2′,3′:4,5]ピロロ[2,3-d]ピリダジン-5(6H)-オン 化学特性,用途語,生産方法

• 説明

  Pyruvate kinase catalyzes the final step in glycolysis, the formation of pyruvate and ATP from phosphoenolpyruvate and ADP. The expression of the M₂ isozyme of pyruvate kinase (PKM2) plays an important role in the metabolic reprogramming of tumor cells, which require high amounts of glucose for proliferation. PKM2 is allosterically regulated by the upstream glycolytic intermediate, fructose-1,6-bisphosphate (FBP), which controls glycolysis in a feed forward mechanism. Whereas cancer cells exist in highly phosphorylated states, the binding of certain peptide motifs with phosphorylated tyrosines can inhibit PKM2 activity by causing the release of FBP from the allosteric site. ML-265 activates tumor-specific PKM2 (EC₅₀ = 92 nM) by binding to the dimer-dimer interface between two subunits of PKM2 and inducing tetramerization, which is the most active form of the enzyme. It demonstrates >100-fold selectivity for PKM2 over the related PKM1, PKR, and PKL isoforms. At 50 mg/kg, ML-265 has been shown to reduce tumor size, weight, and occurrence in mice bearing H1299 cell xenografts in a model of human non-small cell lung carcinoma.

2-(メチルスルフィニル)-4-メチル-6-(3-アミノベンジル)-4H-チエノ[2′,3′:4,5]ピロロ[2,3-d]ピリダジン-5(6H)-オン 生産企業

Global(114)Suppliers

2-(メチルスルフィニル)-4-メチル-6-(3-アミノベンジル)-4H-チエノ[2′,3′:4,5]ピロロ[2,3-d]ピリダジン-5(6H)-オン スペクトルデータ(¹HNMR)