Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ , with an IC 50 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 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 IC 50 of 1 nM. Parsaclisib inhibits the proliferation of human, dog, rat, and mouse primary B cells after activation of these receptors, with IC 50 s ranging from 0.2 to 1.7 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 IC 50 s of ≤10 nM in the four MCL cell lines. Pfeiffer, SU-DHL-5, SU-DHL-6, and WSU-NHL were highly sensitive, with IC 50 s from 2 to 8 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice (5-9 weeks) were inoculated with A20 cellsDosage: 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. Form:Solid IC50& Target:PI3Kδ 1 nM (IC 50 )
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Parsaclisib hydrochloride
CAS number：1995889-48-9 molecular formula：C20H23Cl2FN6O2
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| Chinese alias | 盐酸帕沙克利西 | ||
| English alias | (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one hydrochloride | (R)-4-(3-((S)-1-(4-Amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolid | ||
| CAS number | 1995889-48-9 | molecular formula | C20H23Cl2FN6O2 |
| molecular weight | 469.34 g/mol | Exact mass | ≥98% |
| PSA | 108.000 Ų | logp | - |
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