SGI-1776
爱闪购- SGI 1776;SGI1776
货号: abs812211
货号-规格 | 货期 | 价格 | 数量 |
abs812211-5mg | 现货 | - + | |
abs812211-10mg | 现货 | - + | |
abs812211-50mg | 现货 | - + |

产品描述 | ||
描述 | SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1. | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | SGI 1776;SGI1776 | |
外观 | White to yellow powder | |
可溶性/溶解性 | DMSO : 75 mg/mL (185 mM) Ethanol : 75 mg/mL (185 mM) | |
生物活性 | ||
靶点 | Pim1;FLT3;Pim3;Pim2 | |
In vitro(体外研究) | In addition to Pim, SGI-1776 also potently targets FLT3 (IC50 = 44nM). Treatment of AML cells with SGI-1776 results in a concentration-dependent induction of apoptosis. Importantly, SGI-1776 is also cytotoxic in AML primary cells, irrespective of FLT3 mutation status and results in Mcl-1 protein decline. Treatment of CLL cells with SGI-1776 results in a concentration-dependent induction of apoptosis. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. Apoptosis induction coupled with the inhibition of RNA synthesis is observed in CLL cells treated with SGI-1776. SGI-1776 exhibites cytotoxic activity in vitro with a median relative IC50 of 3.1 mM. SGI-1776 induces tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induces complete responses of subcutaneous MV4;11. | |
In vivo(体内研究) | Consistent with cell line data, xenograft model studies with mice bearing MV-4-11 tumors shows efficacy with SGI-1776. SGI-1776 has shown preclinical activity against leukemia and solid tumor cell line models with IC50 values of 0.005–11.68 mM. SGI-1776 induces significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts. | |
参考文献 | ||
参考文献 | ||
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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