| 应用 |
A potent apoptotic that targets Pim and FLT3 in AML and CLL cells. |
| 产品介绍 |
SGI-1776 free base是一种新型的，ATP竞争性的Pim1抑制剂，IC50为7 nM，比作用于Pim2和Pim3选择性分别高50和10倍，作用于Flt3和haspin也有效。 |
| 备注 |
SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1. |
| 生化机理 |
SGI-1776 is a novel ATP-competitive inhibitor of Pim-1, Pim-2, and Pim-3 (IC50 = 7, 363, and 69 nM, respectively). In addition to inhibiting Pim, this compound also inhibits FLT3 (IC50 = 44 nM). SGI-1776 is also cytotoxic in AML primary cells, regardless of the FLT3 mutation status, which results in Mcl-1 protein decline. SGI-1776 inhibits tumor growth for intermediate EFS T/C activity in 1 of 39 evaluable models. |
| 别名 |
SGI1776; N-[(1-甲基-4-哌啶基)甲基]-3-[3-(三氟甲氧基)苯基]-咪唑并[1,2-b]哒嗪-6-胺;SGI 1776; SGI1776;SGI-1776;N-[(1-Methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine |
