umbralisib (TGR-1202)，1532533-67-7，Moligand™, 10mM in DMSO

中文名：umbralisib (TGR-1202)

英文名：umbralisib (TGR-1202)

纯度：Moligand™, 10mM in DMSO

货号：U421818

Cas号：1532533-67-7

存储温度：-80℃储存

产品介绍：

Information

Umbralisib (TGR-1202, Rp-5264), a novel, next generationPI3Kδinhibitor, inhibits PI3Kδ activity in enzyme and cell based assays withIC50andEC50values of 22.2 & 24.3 nM, respectively.

Targets

PI3Kδ (Cell-free assay) 22.2 nM

In vitro

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

The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.

Cell Research(from reference)

Cell lines：Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells 

Incubation Time：96 h 

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