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SAR407899
PENTOSTATIN| 货号： | RH150006 |
| CAS号： | 1210608-43-7 |
| 规格： | 100mg |
PIM447是一个新颖的pan-PIM抑制剂。
生物活性
PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.
target: pan-PIM inhibitor [2] [3]
In vitro: 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.[1]
In vivo: PIM447 significantly reduces the tumor burden and preventes tumor-associated bone loss in a disseminated murine model of human myeloma.[1]
化学信息
| 分子量 | 440.46 | 储存条件 | 参考CoA中推荐的条件进行储存。 |
|---|---|---|---|
| 分子式 | C₂₄H₂₃F₃N₄O | ||
| CAS号 | 1210608-43-7 | ||
| 溶剂/溶解度 | 10 mM in DMSO |
相关文献
[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
