1532533-67-7
1532533-67-7 structure
- Name: tgr-1202
- Chemical Name: tgr-1202
- CAS Number: 1532533-67-7
- Molecular Formula: C31H24F3N5O3
- Molecular Weight: 571.54900
- Catalog: Research Areas Cancer
- Create Date: 2017-11-10 09:55:43
- Modify Date: 2024-01-14 22:17:07
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Umbralisib (TGR-1202) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib (TGR-1202) is also active against CK1ε, with an EC50 value of 6.0 μM.
| Name | tgr-1202 |
|---|---|
| Synonyms | (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 |
| Description | Umbralisib (TGR-1202) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib (TGR-1202) is also active against CK1ε, with an EC50 value of 6.0 μM. |
|---|---|
| Related Catalog | |
| Target |
PI3Kδ:22.2 nM (IC50) |
| In Vitro | Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, Umbralisib (RP5264; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells[2]. |
| In Vivo | In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, Umbralisib (RP5264; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2]. |
| References |
| Melting Point | 139 - 142 °C |
|---|---|
| Molecular Formula | C31H24F3N5O3 |
| Molecular Weight | 571.54900 |
| Exact Mass | 571.18300 |
| PSA | 109.06000 |
| LogP | 7.24390 |
| Storage condition | -20℃ |