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.
For research use only. We do not sell to patients.
Chemical Information
| Name | TGR-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 |
| Synonyms | RP5264; TGR1202; TGR 1202; RP-5264; RP 5264 |
| Molecular Formula | C31H24F3N5O3 |
| Molecular Weight | 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 Number | 1532533-67-7 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | crystalline solid |
|---|---|
| Purity | 98% |
| Storage | 3 years -20ºCpowder |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Chemical Structure
