[CAS NO. 1532533-67-7] umbralisib (TGR-1202)
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:
PRODUCTS SPECIFICATIONS [1532533-67-7]
Store
Catalog
SLK-S8194
Brand
Selleck
CAS
1532533-67-7
DESCRIPTION [1532533-67-7]
Overview
| MDL | MFCD28386165 |
|---|---|
| Molecular Weight | 571.55 |
| Molecular Formula | C31H24F3N5O3 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7496 mL | 8.7481 mL | 17.4963 mL |
| 5 mM | 0.3499 mL | 1.7496 mL | 3.4993 mL |
| 10 mM | 0.1750 mL | 0.8748 mL | 1.7496 mL |
| 50 mM | 0.0350 mL | 0.1750 mL | 0.3499 mL |
Description
Umbralisib (TGR-1202, Rp-5264), a novel, next generation inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with and values of 22.2 & 24.3 nM, respectively.
Targets
| PI3Kδ [1] (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.
Powered by Arctom Copyright © 2026 Arctom. All rights
reserved.