| Description | Umbralisib (TGR 1202) is a PI3Kδ inhibitor. |
| In vitro | Umbralisib和carfilzomib通过破坏4E-BP1-eIF4F-c-Myc轴线共同协同地杀死血癌细胞。Umbralisib与carfilzomib联合使用时，能够协同并选择性地抑制c-Myc和E2F转录程序。在DLBCL细胞系LY7中，Umbralisib（15-50 μM）强效抑制c-Myc的表达，并且因其结构特征适合针对淋巴瘤细胞中的CK1ε而具有独特性。 |
| In vivo | 在NOD/SCID小鼠的皮下异种移植T细胞急性淋巴细胞白血病（T-ALL）模型中，使用MOLT-4细胞系，TGR-1202（每日150 mg/kg，口服）显著缩小了肿瘤，效果在第25天显现。 |
| Target activity | PI3Kδ:22.2 nM |
| Synonyms | TGR-1202, RP5264, TGR 1202, TGR1202 |
| molecular weight | 571.55 |
| Molecular formula | C31H24F3N5O3 |
| CAS | 1532533-67-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 91 mg/mL (159.2 mM) |
| References | 1. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth. 2. Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99 |