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TGR-1202

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.


 

For research use only. We do not sell to patients.

Chemical Information

NameTGR-1202
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 
SmileNC1=C2C(=NC=N1)N(N=C2C2=CC(=C(C=C2)OC(C)C)F)[C@@H](C)C=2OC1=CC=C(C=C1C(C2C2=CC(=CC=C2)F)=O)F
InChiKeyIUVCFHHAEHNCFT-INIZCTEOSA-N
InChiInChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1
CAS Number1532533-67-7
Related CAS

Ordering Information

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Formulationcrystalline solid 
Purity98% 
Storage3 years -20ºCpowder 
SolubilitySoluble in DMSO 
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study
Not available

Chemical Structure

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

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