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Seletalisib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Seletalisib图片
CAS NO:1362850-20-1
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品名称
UCB5857
产品介绍
Seletalisib 是一种有效的、选择性的PI3Kδ抑制剂,其 IC50=12 nM。

产品描述

Seletalisib (UCB5857) is a potent and specific PI3Kδ inhibitor (IC50: 12 nM).

体外活性

Seletalisib is able to block AKT phosphorylation following activation of the BCR in a B-cell line. No indications of cytotoxicity are observed in PBMCs or other cell types treated with Seletalisib. Seletalisib blocks human T-cell production of several cytokines from activated T-cells. Seletalisib inhibits T-cell differentiation to Th1, Th2, and Th17 subtypes. Additionally, Seletalisib inhibits B-cell proliferation and cytokine release. In human whole blood assays, Seletalisib inhibits CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation.

体内活性

Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat. The inhibition is observed at all tested doses of Seletalisib with almost complete inhibition reached at dose levels ≥1 mg/kg. Seletalisib has potent in vivo effects with an estimated IC50 value of<10 nM.

细胞实验

Seletalisib is dissolved 1 mM solution in DMSO, and tested in a concentration-response, to explore the effects of PI3Kδ-specific inhibition compared with complete inhibition of class I PI3K signaling. In addition, seletalisib is tested in the BioMap BT cell system at concentrations of 1000, 100, 10, and 1 nM. An activity profile is generated based on the effect of the compounds on the levels of cellular readouts, including cytokines, growth factors, adhesion molecules, and proliferation endpoints.

动物实验

Rats are dosed with Seletalisib (0.1-10 mg/kg in 500 μL volume) or vehicle via oral gavage 30 min prior to i.v. administration of anti- CD3 antibody administered in a 200 μL dose volume. The vehicle is methylcellulose or saline for oral and i.v. administration, respectively. Seletalisib levels and IL-2 levels are measured.

Cas No.

1362850-20-1

分子式

C23H14ClF3N6O

分子量

482.85

别名

UCB5857

储存和溶解度

DMSO:80 mg/mL (165.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years