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
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描述 |
PCI 29732是一种选择性的、不可逆的Btk抑制剂，IC50为0.5 nM。 |
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靶点 |
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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. |
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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. |
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动物实验 |
Animal Models: Arthritic DBA/1 mice |
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 |
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1 mM |
2.6923 mL |
13.4615 mL |
26.9230 mL |
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5 mM |
0.5385 mL |
2.6923 mL |
5.3846 mL |
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10 mM |
0.2692 mL |
1.3461 mL |
2.6923 mL |
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50 mM |
0.0538 mL |
0.2692 mL |
0.5385 mL |
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