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Parsaclisib hydrochloride

產(chǎn)品活性：Parsaclisib hydrochloride (INCB050465 hydrochloride) 是一種有效，選擇性和具有口服活性的 PI3Kδ 抑制劑，IC₅₀ 值為 1 nM。Parsaclisib hydrochloride 相對(duì)于其他 PI3K I 類同工型的選擇性約為 20000 倍。Parsaclisib hydrochloride 可用于研究復(fù)發(fā)或難治性 B 細(xì)胞惡性腫瘤。

研究領(lǐng)域：PI3K/Akt/mTOR

作用靶點(diǎn)：PI3K

In Vitro: Parsaclisib (0.1-3000 nM; 4 d) inhibits proliferation of MCL and DLBCL cell lines.
Parsaclisib (0.1-1000 nM; 2 h) inhibits anti-IgM-induced pAKT (Ser473) in the Ramos Burkitt’s lymphoma cell line, with an IC₅₀ of 1 nM.
Parsaclisib inhibits the proliferation of human, dog, rat, and mouse primary B cells after activation of these receptors, with IC₅₀s ranging from 0.2 to 1.7 nM.

In Vivo: Parsaclisib (10 mg/kg; oral gavage twice daily for 7-19 days) inhibits tumor growth in the BALB/c mice bearing the A20 murine lymphoma cells.
Parsaclisib (0.1-10 mg/kg; p.o. twice daily) slows Pfeiffer xenograft tumor growth in a dose-dependent manner. And Parsaclisib was well tolerated.
Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473) in Pfeiffer subcutaneous mouse xenograft models.

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