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Catalog No.: 611904
Cas No.: 1532533-67-7
Purity : 98% 

TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3K activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

TGR-1202 displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, TGR-1202 causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 resulted initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrated that TGR-1202 caused a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells. Further, the compound exhibited good oral absorption with favourable pharmacokinetic properties in rodents.


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Chemical Information

Iupac Chemical Name(S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one 
SynonymsRP5264; TGR1202; TGR 1202; RP-5264; RP 5264 
Molecular FormulaC31H24F3N5O3 
Molecular Weight571.55 
CAS Number1532533-67-7
Related CAS

Ordering Information

PackagingPriceAvailabilityPurityShipping Time
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Formulationcrystalline solid 
Storage3 years -20ºCpowder 
SolubilitySoluble in DMSO 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
HS Code
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Cell study
Animal study
Clinical study
Not available

Chemical Structure

611904 - TGR-1202 | CAS 1532533-67-7

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