| Identification | Back Directory | [Name]
Parsaclisib | [CAS]
1426698-88-5 | [Synonyms]
Parsaclisib
Parsaclisib(INCB050465)
(4R)-4-{3-[(1S)-1-{4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl}ethyl]-5-chloro-2-ethoxy-6-fluorophenyl}pyrrolidin-2-one
2-Pyrrolidinone, 4-[3-[(1S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl]-, (4R)-
inhibit,INCB-050465,Parsaclisib,Phosphoinositide 3-kinase,relapsed,INCB 050465,refractory,malignancies,PI3K,Inhibitor,PI3Kδ,B-cell | [Molecular Formula]
C20H22ClFN6O2 | [MDL Number]
MFCD31692358 | [MOL File]
1426698-88-5.mol | [Molecular Weight]
432.88 |
| Chemical Properties | Back Directory | [Boiling point ]
650.9±55.0 °C(Predicted) | [density ]
1.54±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (288.76 mM) | [form ]
Solid | [pka]
15?+-.0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies[1][2][3]. | [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[2].
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[2].
Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473) in Pfeiffer subcutaneous mouse xenograft models[2]. | Animal Model: | Female BALB/c mice (5-9 weeks) were inoculated with A20 cells[2] | | 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. |
| [IC 50]
PI3Kδ: 1 nM (IC50) | [References]
[1] Niu Shin, et al. Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. Cancer Research. 2015, Aug. 75(15).
[2] Shin N, et, al. Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222. DOI:10.1124/jpet.120.265538
[3] Yue EW, et, al. INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ). ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560. DOI:10.1021/acsmedchemlett.9b00334 |
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| Company Name: |
Syntechem Co.,Ltd.
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| Tel: |
519-88298820 15861130028 |
| Website: |
http://www.syntechem.com |
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