全部商品分类首页
Umbralisib
.jpg)
1/2
用小程序，查商品更便捷
产品介绍
产品介绍
产品信息
抗原名称
PI3Kδ
商品描述
Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach.
分子量
571.560
纯度
98%
可溶性
10 mM in DMSO
In vitro(体外研究)
The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.
In vivo(体内研究)
The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.
背景
分子式
C31H24F3N5O3
CAS号
1532533-67-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
声明 ：本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。