Parsaclisib
- Product Name
- Parsaclisib
- CAS No.
- 1426698-88-5
- Chemical Name
- Parsaclisib
- Synonyms
- Parsaclisib;Parsaclisib(INCB050465);Parsaclisib, 10 mM in DMSO;(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
- CBNumber
- CB54668326
- Molecular Formula
- C20H22ClFN6O2
- Formula Weight
- 432.88
- MOL File
- 1426698-88-5.mol
Parsaclisib Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0033435
- Product name
- Parsaclisib
- Purity
- 99.31%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0033435
- Product name
- Parsaclisib
- Purity
- 99.31%
- Packaging
- 10mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- CS-0033435
- Product name
- Parsaclisib
- Purity
- 99.31%
- Packaging
- 25mg
- Price
- $1750
- Updated
- 2021/12/16
- Product number
- CS-0033435
- Product name
- Parsaclisib
- Purity
- 99.31%
- Packaging
- 50mg
- Price
- $2750
- Updated
- 2021/12/16
- Product number
- CS-0033435
- Product name
- Parsaclisib
- Purity
- 99.31%
- Packaging
- 100mg
- Price
- $3950
- Updated
- 2021/12/16
Parsaclisib Chemical Properties,Usage,Production
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
Parsaclisib Preparation Products And Raw materials
Raw materials
Preparation Products
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