产品说明书

PRT062607 HCl

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Chemical Structure| 1370261-97-4 同义名 : P505-15 Hydrochloride;BIIB057;PRT-2607;PRT062607 Hydrochloride
CAS号 : 1370261-97-4
货号 : A224641
分子式 : C19H24ClN9O
纯度 : 99%+
分子量 : 429.907
MDL号 : MFCD25976708
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(81.41 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(116.3 mM)
动物实验配方：

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • Syk

    Syk, IC50:1 nM

  • MLK1

    MLK1, IC50:88 nM
描述 PRT062607 (P505-15) is a novel, highly specific, and potent orally available small-molecule inhibitor of Syk. A FRET assay demonstrates a half-maximal inhibition concentration for Syk at 6±0.2 nM, with a similar inhibitory capacity observed in a radioactive enzyme test, showing a Syk IC50 of 2.1±0.4 nM. In human whole blood, PRT062607 effectively blocks B cell antigen receptor-driven B cell signaling and activation (with IC50 values of 0.27 and 0.28 μM, respectively) and inhibits Fcε receptor 1-triggered basophil degranulation (IC50 of 0.15 μM)[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
C57BL/6 mouse bone marrow cells Cytotoxic assay 5 h Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis, IC50=5.853 μM 25633741
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assay, IC50=8.6 μM 25633741
human Ramos cells Function assay Inhibition of SYK in human Ramos cells, IC50=0.223 μM 23350847
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.63mL

2.33mL

1.16mL

23.26mL

4.65mL

2.33mL
参考文献

[1]Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9.