上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
PIM447 (Synonyms: LGH447)
PIM447 (LGH447) 是一种有效的、口服的、选择性的泛 PIM 激酶抑制剂，对 PIM1、PIM2 和 PIM3 的 Ki 值分别为 6、18 和 9 pM。PIM447 具有双重抗肿瘤和骨保护作用。PIM447 诱导细胞凋亡。
PIM447 Chemical Structure
CAS No. : 1210608-43-7
| 规格 |
|
是否有货 |
|
| 100 mg |
|
询价 |
|
| 250 mg |
|
询价 |
|
| 500 mg |
|
询价 |
|
* Please select Quantity before adding items.
PIM447 的其他形式现货产品:
PIM-447 dihydrochloride (1S,3R,5R)-PIM447 dihydrochloride
| 生物活性 |
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis[1][2].
|
体外研究
(In Vitro) |
PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells[2].
PIM447 (10 μM; 6-24 hours) induces apoptosis[2].
PIM447 (0.1-10 μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (S and G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
| Cell Line: |
MM1S, MM1R, RPMI-8226, MM144, U266, NCI-H929, OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7 cells |
| Concentration: |
0.05, 0.1, 0.5, 1, 5, 10 μM |
| Incubation Time: |
24, 48, 72 hours |
| Result: |
Sensitive cell lines with IC50 values at 48 hours ranging from 0.2 to 3.3 μM (MM1S, MM1R, RPMI-8226, MM144, U266, and NCI-H929) and less sensitive cell lines with IC50 values at 48 hours >7 μmol/L (OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7). |
Western Blot Analysis[2]
| Cell Line: |
MM1S cells |
| Concentration: |
10 μM |
| Incubation Time: |
6, 12, 24 hours |
| Result: |
Promoted the cleavage of initiator caspases, such as caspases 8 and 9, and also the cleavage of the effector caspases 3 and 7, together with PARP cleavage. |
|
体内研究
(In Vivo) |
PIM447 (100 mg/kg; p.o.; 5 times for a week) reduces tumor burden[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
6-week-old female NOD-SCID-IL-2Rγ−/− (NSG) mice (bearing RPMI-8226-luc cells)[2] |
| Dosage: |
100 mg/kg |
| Administration: |
p.o.; 5 times for a week |
| Result: |
Clearly controlled tumor progression as measured by bioluminescence. |
|
| Clinical Trial |
|
| 分子量 |
|
| Formula |
|
| CAS 号 |
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
|
| 参考文献 |
-
[1]. 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.
[2]. 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.
[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
|
所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务
