| Identification | Back Directory | [Name]
N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide | [CAS]
1820565-69-2 | [Synonyms]
EOS-62253
PIM-447 2HCl
LGH-447 dihydrochloride
PIM-447 (dihydrochloride) | [Molecular Formula]
C24H23F3N4O | [MDL Number]
MFCD30489747 | [MOL File]
1820565-69-2.mol | [Molecular Weight]
440.461 |
| Hazard Information | Back Directory | [Uses]
PIM447 dihydrochloride (LGH447 dihydrochloride) 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 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis[1][2]. | [in vivo]
PIM447 (oral gavage; 100 mg/kg; 5 times/week) clearly controlls tumor progression and the serum levels of hIgλ secreted by RPMI-8226-luc cells in mouse model of bone marrow-disseminated human multiple myeloma[1]. | Animal Model: | RPMI-8226-luc cells are injected intravenously into 6-week-old female NODSCID-IL-2Rγ-/-(NSG) mice[1] | | Dosage: | 100 mg/kg | | Administration: | oral gavage; 100 mg/kg; 5 times/week | | Result: | Was well tolerated, as the body weight of mice did not decrease by more than 10%.
Increased bone volume density and trabecular number and reduced trabecular separation relative to vehicle group. |
| [IC 50]
PIM1; PIM2; PIM3 | [References]
[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. DOI:10.1158/1078-0432.CCR-16-0230
[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. DOI:10.1021/acs.jmedchem.5b01275
[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 DOI:10.18632/oncotarget.11457 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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