Cerdulatinib (PRT062070, PRT2070)

Cerdulatinib (PRT062070, PRT2070)CAS号: 1369761-01-2分子式: C20H28ClN7O3S分子量: 482描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述
Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:43 mg/mL warmed (89.21 mM)
生物活性
靶点
TYK2 ,MST1 ,ARK5 ,MLK1 ,Fms
In vitro(体外研究)
In human whole blood from normal donors, Cerdulatinib affects BCR-mediated B-cell activation by dual inhibition of SYK and JAK. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduces cell viability in a subset of NHL cell lines, and induces apoptosis in BCR-signaling competent NHL cell lines.
In vivo(体内研究)
In a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg p.o.) significantly improves inflammatory infiltrate within the synovium and the integrity of the articular cartilage. In addition, Cerdulatinib also blocks BCR-induced B-cell activation and splenomegaly in mice.
参考文献
参考文献
  • 1. Coffey G, J Pharmacol Exp Ther. 2014, 351(3), 538-548.