PIM447
- LGH447
货号: abs818999
货号-规格 | 货期 | 价格 | 数量 |
abs818999-5mg | 4周 | ¥3859.00 | - + |
abs818999-10mg | 4周 | ¥5513.00 | - + |

产品描述 | ||
描述 | PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.target: pan-PIM inhibitor. | |
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 | LGH447 | |
外观 | powder | |
可溶性/溶解性 | Soluble in DMSO | |
生物活性 | ||
靶点 | Pim | |
In vitro(体外研究) | PIM447 is cytotoxic for myeloma cells due to cell cycle disruption and induction of apoptosis mediated by a decrease in phospho-Bad (Ser112) and c-Myc levels and the inhibition of mTORC1 pathway. PIM447 also inhibits in vitro osteoclast formation and resorption, downregulates key molecules involved in these processes and partially disrupts the F-actin ring, while increasing osteoblast activity and mineralization. | |
In vivo(体内研究) | PIM447 significantly reduces the tumor burden and preventes tumor-associated bone loss in a disseminated murine model of human myeloma. | |
参考文献 | ||
参考文献 | [1]. Paíno T et al. The novel pan-PIM kinase inhibitor, PIM447, displays dual anti-myeloma and bone protective effects, and potently synergizes with current standards of care. Clin Cancer Res. 2016 Jul 20. [2]. Burger MT et al. Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. J Med Chem. 2015 Nov 12;58(21):8373-86. [3]. Peters TL et al. Control of translational activation by PIM kinase in activated B-cell diffuse large B-cell lymphoma confers sensitivity to inhibition by PIM447. Oncotarget. 2016 Aug 20 | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
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