Parsaclisib

SKU: orb1218831

Description

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

Key Properties

• CAS Number: 1426698-88-5
• MW: 432.88
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂ClFN₆O₂
• SMILES: CCOc(c([C@H](C)n1nc(C)c2c(N)ncnc12)c1)c([C@@H](C2)CNC2=O)c(F)c1Cl
• Target: PI3K
• Solubility: DMSO:122 mg/mL (281.83 mM; Need ultrasonic)

Bioactivity

• 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. 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.
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• 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. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

INCB050465

Quick Database Links

Gene Symbol

PI3K