货号	价格	上海	北京	珠海	重庆	武汉
V49230-1mg	￥1750.00 V49230-1mg ￥1750.00 3-5天	0 货期：3-5天	-	-	-	-
V49230-5mg	￥3880.00 V49230-5mg ￥3880.00 3-5天	0 货期：3-5天	-	-	-	-
V49230-10mg	￥6210.00 V49230-10mg ￥6210.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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.

体外研究：

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.

体内研究：

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.

参考文献：

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.

保存条件：

2-8°C, 氮气保存

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.131 ml	10.653 ml	21.307 ml
5 mM	0.426 ml	2.131 ml	4.261 ml
10 mM	0.213 ml	1.065 ml	2.131 ml
50 mM	0.043 ml	0.213 ml	0.426 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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