Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of casein kinase 1 epsilon;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta
Product Description
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
Product Properties
ALogP
6.393
HBD Count
1
Rotatable Bond
6
Associated Targets(Human)
CSNK1ETclinCasein kinase I isoform epsilon (1 Activities)
1.Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J, Hao Y, Xu X, Deng SX et al.. (2017) Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.. Blood, 129 (1):(88-99). [PMID:27784673][10.1021/op500134e]
2.Burris 3rd HA, Flinn IW, Patel MR, Fenske TS, Deng C, Brander DM, Gutierrez M, Essell JH, Kuhn JG, Miskin HP et al.. (2018) Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study.. Lancet Oncol, 19 (4):(486-496). [PMID:29475723][10.1021/op500134e]
3.Barrientos JC. (2018) Can umbralisib bring PI3Kδ out of the shadows?. Lancet Oncol, 19 (4):(432-434). [PMID:29475725][10.1021/op500134e]
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H2206124