PCI 29732

¥800.00¥2,000.00

CAS 号: 330786-25-9
英文名字:PCI 29732
质量标准:>98%,BR
货号: MB0389

PCI 29732
分子式:C22H21N5O分子量:371.43

简介:PCI 29732是一种选择性的、不可逆的Btk抑制剂,IC50为0.5 nM。
物理性状及指标:
外观:……………………粉末
溶解性:…………………DMSO: 74 mg/mL (199.23 mM);Ethanol:4 mg/mL (10.77 mM);Water:Insoluble
含量:……………………>98%
储存温度:-20℃,避光防潮密闭干燥

生物活性

描述

PCI 29732是一种选择性的、不可逆的Btk抑制剂,IC50为0.5 nM。

靶点

BTK (Cell-free assay)

BLK (Cell-free assay)

Bmx (Cell-free assay)

EGFR (Cell-free assay)

YES (Cell-free assay)

0.5 nM

0.5 nM

0.8 nM

5.6 nM

6.5 nM

体外

PCI-32765 blocks BCR signaling in human peripheral B cells at concentrations that does not affect T cell receptor signaling. In DOHH2 cells, PCI-32765 inhibits autophosphorylation of Btk (IC50, 11 nM), phosphorylation of Btk’s physiological substrate PLCγ(IC50, 29 nM), and phosphorylation of a further downstream kinase, ERK (IC50, 13 nM). PCI-32765 is more than 1,000-fold selective for inhibition of antigen receptor signaling in B cells over T cells, and that only B-cell inhibition is sustained following short duration treatment.

体内

In mice with collagen-induced arthritis, orally administered PCI-32765 reduces the level of circulating autoantibodies and completely suppresses disease. PCI-32765 also inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. The mean terminal plasma half-life of PCI-32765 following oral dosing in mice is 1.7 to 3.1 h.

动物实验

Animal Models:Arthritic DBA/1 mice
Formulation:–
Dosages:3.125, 12.5, or 50 mg/kg per day
Administration:oral
(Only for Reference)

储液配置及储存:按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-60°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃1-3月;-80℃ 3-6月。

浓度/体积/质量

1 mg

5 mg

10 mg

1 mM

2.6923 mL

13.4615 mL

26.9230 mL

5 mM

0.5385 mL

2.6923 mL

5.3846 mL

10 mM

0.2692 mL

1.3461 mL

2.6923 mL

50 mM

0.0538 mL

0.2692 mL

0.5385 mL

●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。

●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,以上数据仅供参考交流研究之用。

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规格

2mg, 10mg

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