TGR-1202
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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化学信息
| 名称 | TGR-1202 |
|---|---|
| Iupac 化学名称 | (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 |
| 同义词 | RP5264; TGR1202; TGR 1202; RP-5264; RP 5264 |
| 英文同义词 | RP5264; TGR1202; TGR 1202; RP-5264; RP 5264 |
| 分子式 | C31H24F3N5O3 |
| 分子量 | 571.55 |
| Smile | NC1=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 |
| InChiKey | IUVCFHHAEHNCFT-INIZCTEOSA-N |
| InChi | InChI=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号 | 1532533-67-7 |
| 相关CAS号 |
订购信息
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