All AbMole products are for research use only, cannot be used for human consumption.
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.
In vitro: Umbralisib (TGR-1202) displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, Umbralisib (TGR-1202) 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. Umbralisib (TGR-1202) causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.
In vivo: Umbralisib (TGR-1202) exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.
| Cell Experiment | |
|---|---|
| Cell lines | Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells |
| Preparation method | Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay. |
| Concentrations | |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | Female Balb/c mice |
| Formulation | |
| Dosages | 12.5, 25, 50 mg/kg |
| Administration | p.o. |
| Molecular Weight | 571.55 |
| Formula | C31H24F3N5O3 |
| CAS Number | 1532533-67-7 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
