性能参数

产品名称

PF 543 hydrochloride

规格

10 mg 50 mg

货号

GOY-Y2658

 含量

>98.00%

CAS

1706522-79-3

别名

N/A

化学名

N/A

分子式

C27H31NO4S.HCl

分子量

分子量 502.07

溶解度

DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

Potent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. Suppresses HCT-116 tumor xenograft growth in mice. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.

Ju et al (2016) Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543. Biochem.Biophys.Res.Commun. 470 728 PMID:26775841 |Schnute et al (2012) Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem.J. 444 79 PMID:22397330 |Schnute et al (2017) Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits J.Med.Chem. 60 2562 PMID:28231433 |Zhang et al (2014) Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J.Clin.Invest. 124 2750 PMID:24837436

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乙二胺四乙酸  99.99% metals basis  茚并(1,2,3-cd)芘标准溶液 10～100μg/mL,基体：甲醇

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