Parsaclisib HCl

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 HCl 是一种具有抗肿瘤活性的选择性 PI3Kδ 抑制剂。 Parsaclisib 表现出有效的活性，IC50 值范围为 0.2 至 2 nM。

Parsaclisib HCl is a selectve PI3Kδ inhibitor with antitumor activity. Parsaclisib demonstrates potent activity with IC50 values ranging from 0.2 to 2 nM.

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 AssayCell 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+CD44 high and CD8+CD44 high T cells in both spleens and tumors.

INCB50465 HCl | INCB-50465 | INCB 50465 | INCB050465 HCl | INCB-050465 | INCB 050465

PI3K/Akt/mTOR signaling

PI3K

PI3Kδ

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1995889-48-9

469.34

C20H23Cl2FN6O2

>98% (HPLC)

DMSO:90 mg/mL(191.76 mM);Water:Insoluble

O=C1NC[C@@H](C2=C(F)C(Cl)=CC([C@@H](N3N=C(C)C4=C(N)N=CN=C43)C)=C2OCC)C1.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years