TGR-1202

Catalog No.S8194 Synonyms: Rp-5264

TGR-1202 Chemical Structure

Molecular Weight(MW): 571.55

TGR-1202, 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.

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Biological Activity

Description TGR-1202, 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.
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[1].

In vivo The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile[1].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells
  • Concentrations: --
  • Incubation Time: 96 h
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female Balb/c mice
  • Formulation: --
  • Dosages: 12.5, 25, 50 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (174.96 mM)
Ethanol 7 mg/mL warmed (12.24 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+2% Tween 80+H2O
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 571.55
Formula

C31H24F3N5O3

CAS No. 1532533-67-7
Storage powder
Synonyms Rp-5264

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID