PIM447是泛PIM激酶抑制剂，对PIM1，PIM2，PIM3的 Ki 分别为6，18，9 nM。
| Cas No. | 1820565-69-2 |
| 别名 | LGH447 dihydrochloride |
| Canonical SMILES | O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=C([C@H]4C[C@@H](N)C[C@@H](C)C4)C=CN=C3.Cl.Cl |
| 分子式 | C24H25Cl2F3N4O |
| 分子量 | 513.38 |
| 溶解度 | DMSO: ≥ 46.7 mg/mL (90.97 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PIM447 is a pan-PIM kinase ihibitor with Kis of 6, 18, 9 nM for PIM1, PIM2 and PIM3, respectively. [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 |
