产品
编 号:F246976
分子式:C20H23Cl2FN6O2
分子量:469.34
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1mg
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5mg
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10mg
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生物活性:
Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies.

体内研究:
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.Animal Model:Female BALB/c mice (5-9 weeks) were inoculated with A20 cells
Dosage:10 mg/kg
Administration:Oral gavage twice daily for 7-19 days
Result:Resulted in significant tumor growth inhibition (TGI).Reduced the percentage of Tregs (CD4+CD25+FOXP3+) in tumors and spleens.Increased the ratio of CD4+ and CD8+ T cells to Tregs in spleens and tumors.Decreased the number of CD4+CD44high and CD8+CD44high T cells in both spleens and tumors.

体外研究:
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.
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