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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 |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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