Umbralisib

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

Umbralisib Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach. 

• Verwenden

  RP 5264 is a novel PI3K inhibitor that enhances Brentuximab Vedotin-induced lymphoma cell death.

• Trademarks

  Ukonig

• Allgemeine Beschreibung

  Class: lipid kinase; Treatment: MZL, FL; Other name: TGR-1202; Elimination half-life = 91 h; Protein binding > 99.7%

• Pharmakokinetik

  Umbralisib has a prolonged half-life of 91 h, which enables once-daily dosing. However, the recommended dosage of 800 mg is the highest among all the PI3K inhibitors in use, presumably due to its limited oral bioavailability.

• Synthese

  The synthesis of Umbralisib is as follows:
  To a solution of intermediate 13 (0.134 g, 0.494 mmol) in THF (2.0 ml), intermediate 5 (0.150 g, 0.494 mmol) and triphenylphosphine (0.194 g, 0.741 mml) were added and stirred at RT for 5 min. Diisopropylazodicarboxylate ( 0.15 ml, 0.749 mmol) was added heated to 45°C. After 2h, the reaction mixture was quenched with with water and extracted with ethyl acetate. The organic layer was dried over sodium sulphate and concentrated under reduced pressure. The crude product was purified by column chromatography with ethyl acetate : petroleum ether to afford Umbralisib as an off-white solid (0.049 g, 20 %).
  

• target

  PI3Kδ, CK1ε

Umbralisib Upstream-Materialien And Downstream Produkte

Umbralisib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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