Catalog No.S8194 Synonyms: Rp-5264
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.
Purity & Quality Control
Choose Selective PI3K Inhibitors
|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.|
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.|
|In vitro||DMSO||100 mg/mL warmed (174.96 mM)|
|Ethanol||7 mg/mL warmed (12.24 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+H2O
For best results, use promptly after mixing.
* 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.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03207256||Enrolling by invitation||Chronic Lymphocytic Leukemia|Non Hodgkin Lymphoma||TG Therapeutics Inc.||June 28 2017||Phase 2|
|NCT03283137||Recruiting||CLL|B-cell Non Hodgkin Lymphoma||University of Chicago||January 23 2018||Phase 1|
|NCT02874404||Active not recruiting||Recurrent Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma||Matthew Lunning DO|National Cancer Institute (NCI)|University of Nebraska||October 2016||Phase 2|
|NCT02793583||Recruiting||Diffuse Large B-Cell Lymphoma|Follicular Lymphoma|Marginal Zone Lymphoma|Small Lymphocytic Lymphoma|Mantle Cell Lymphoma||TG Therapeutics Inc.||June 2016||Phase 2|Phase 3|
|NCT02742090||Recruiting||Chronic Lymphocytic Leukemia||TG Therapeutics Inc.||April 2016||Phase 2|
|NCT02656303||Recruiting||Chronic Lymphocytic Leukemia||TG Therapeutics Inc.||January 2016||Phase 2|
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.
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