PIM-447 dihydrochloride (Synonyms: LGH447 dihydrochloride) |
رقم الكتالوجGC36918 |
ثنائي هيدروكلوريد PIM447 (LGH447 ثنائي هيدروكلوريد) هو مثبط قوي ، ومتوفر عن طريق الفم ، وانتقائي كيناز بان-بيم ، بقيم Ki تبلغ 6 و 18 و 9 مساءً لـ PIM1 و PIM2 و PIM3 ، على التوالييعرض ثنائي هيدروكلوريد PIM447 تأثيرات مزدوجة مضادة للورم النخاعي وتأثيرات واقية للعظامثنائي هيدروكلوريد PIM447 يحث على موت الخلايا المبرمج
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Cas No.: 1820565-69-2
Sample solution is provided at 25 µL, 10mM.
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
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