Parsaclisib hydrochloride (INCB050465 hydrochloride) 是一种有效，选择性和具有口服活性的 PI3Kδ 抑制剂，IC50 值为 1 nM。Parsaclisib hydrochloride 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib hydrochloride 可用于研究复发或难治性 B 细胞恶性肿瘤。
货号:ajcx34030
CAS:1995889-48-9
分子式:C20H23Cl2FN6O2
分子量：469.34
溶解度:DMSO : 240 mg/mL (511.36 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 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[1][2][3].

Parsaclisib (0.1-3000 nM; 4 d) inhibits proliferation of MCL and DLBCL cell lines[2].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[2].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[2].

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].

[1]. Shin N, 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.
[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.