Parsaclisib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Parsaclisib 是一种有效的选择性 PI3Kδ 抑制剂（在 1 mM ATP 下，IC50 为 1 nM）。

Parsaclisib is a potent and selective inhibitor of PI3Kδ(IC50 of 1 nM at 1 mM ATP).

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. Cell Proliferation Assay Cell Line:Jeko-1, Mino, JVM2, Rec-1, Pfeiffer, SU-DHL-5, SU-DHL-6, WSU-NHL, SU-DHL-4, SU-DHL-8, and WILL-2 cells Concentration:0.1-3000 nM Incubation Time:4 days Result:Resulted in a maximal inhibition of 70-90%, with IC50s of ≤10 nM in the four MCL cell lines.Pfeiffer, SU-DHL-5, SU-DHL-6, and WSU-NHL were highly sensitive, with IC50s from 2 to 8 nM.

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.

INCB050465

PI3K/Akt/mTOR signaling

PI3K

PI3Kδ

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1426698-88-5

432.88

C20H22ClFN6O2

>98% (HPLC)

DMSO:122 mg/mL?(281.83 mM;?Need ultrasonic)

CCOc(c([C@H](C)n1nc(C)c2c(N)ncnc12)c1)c([C@@H](C2)CNC2=O)c(F)c1Cl

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(-20℃)

With Ice Pack

≥ 2 years