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Parsaclisib

(Synonyms: INCB050465; IBI-376)

目录号: PL09804 纯度: ≥99%

Parsaclisib (INCB050465) 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 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib 可用于研究复发或难治性 B 细胞恶性肿瘤。

CAS No. :1426698-88-5

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中文名称	Parsaclisib
英文名称	Parsaclisib
英文别名	Parsaclisib;INCB050465;Parsaclisib free base;OS7097575K;(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;(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;Parsaclisib [INN];Parsaclisib [USAN];Parsaclisib (USAN/INN);Parsaclisib [USAN:INN];INCB050465 free base
Cas No.	1426698-88-5
分子式	C₂₀H₂₂ClFN₆O₂
分子量	432.88
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Parsaclisib (INCB050465) 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 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib 可用于研究复发或难治性 B 细胞恶性肿瘤。

产品详情

Parsaclisib (INCB050465) 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 相对于其他 PI3K I 类同工型的选择性约为 20000 倍。Parsaclisib 可用于研究复发或难治性 B 细胞恶性肿瘤。

生物活性

Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC 50 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.

性状

Solid

IC50 & Target[1][2]

PI3Kδ 1 nM (IC50)

体外研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (288.76 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Parsaclisib

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