首页 Immunology/Inflammation Antiviral PF06650833
PF06650833
编号 TQ0167    
CAS 1817626-54-2     分子式 C18H20FN3O4     分子量 361.37
靶点:
PF06650833 is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).
选择批次  
纯度 98.00%
规格 库存 单价 数量
25 mg 上海现货 2900.00
50 mg 上海现货 5200.00
100 mg 上海现货 9400.00
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生物活性

产品描述

PF06650833 is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).

靶点活性

体外活性

The kinome selectivity profile of PF06650833 (Compound 40) is assessed in a panel of 278 kinases at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4. Lactam PF06650833 is assessed in a whole-cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to and including 30 μM. In a voltage clamp assay, PF06650833 inhibits hERG current by 25% at 100 μM.

体内活性

PF06650833 (0.3-30 mg/kg; p.o; for 2.5 hours; male SD rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of PF06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF06650833 at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of PF06650833 is 0.3.

动物实验

Animal Model: Male Sprague-Dawley rats Dosage: 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg Administration: Oral administration; for 2.5 hours

化学信息

分子量

361.37

分子式

C18H20FN3O4

CAS

1817626-54-2

溶解度

DMSO: 30 mg/mL (83.02 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.767 ml 13.836 ml 27.672 ml
5 mM 0.553 ml 2.767 ml 5.534 ml
10 mM 0.277 ml 1.384 ml 2.767 ml
50 mM 0.055 ml 0.277 ml 0.553 ml
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