LGH447 dihydrochloride MedChemExpress (MCE)

Product Name	PIM-447 (dihydrochloride)
Synonyms	EOS-62253;PIM-447 2HCl;PIM447 DIHYDROCHLORIDE;LGH-447 dihydrochloride;PIM-447 (dihydrochloride);N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
CAS	1820565-69-2
EINECS
Chemical Formula	C24H23F3N4O
Molecular Weight	440.4608296
inchi
Package	10 mM * 1 mL;10 mM * 1 mL;1 mg;1 mg;5 mg;5 mg;10 mg;10 mg
Price	Email to quote
Descriptions	PIM-447 dihydrochloride PIM-447 dihydrochloride MedChemExpress (MCE) HY-19322B 1820565-69-2 LGH447 dihydrochloride 99.94% 4°C, sealed storage, away from moisture In solvent : -80°C, 1 year Descriptions PIM-447 dihydrochloride PIM-447 dihydrochloride MedChemExpress (MCE) HY-19322B 1820565-69-2 LGH447 dihydrochloride 99.94% 4°C, sealed storage, away from moisture In solvent : -80°C, 1 year -20°C, 6 months (sealed storage, away from moisture) Room temperature in continental US may vary elsewhere. 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. PIM-447?(0.05-10 μM 24, 48 and 72 hours) has inhibitory effects in MM cells, it against sensitive cell lines with IC50 values 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 h >7 μM (OPM-2, RPMI-LR5, U266-Dox4 and U266-LR7)[1].PIM-447?(0.1-10 μM 24, 48 and 72 hours) does not induce important levels of apoptosis, when PIM447 at 5 μM, it substantially increases annexin-V levels (about 30%) in sensitive cell lines(MM1S, NCI-H929 and RPMI-8226). When PIM447 at 10 μM, it induces apoptosis in all the cell lines but to a lesser extent in OPM-2 and RPMI-LR5[1].PIM447 promotes the cleavage of initiator caspases, such as caspases 8 and 9, and increases the cleavage of the effector caspases 3 and 7, together with PARP cleavage in MM1S,RPMI-8226 and NCI-H929 cells[1].PIM447 (0.1-1 μM) increases the percentage of cells in the G0/G1 phase and decreases the proliferative phases (S and G2/M) of the cell cycle. The effects at low concentrations (0.1-1 μM) were more pronounced in MM1S cells than in OPM-2[1]. 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]. PIM1 PIM2 PIM3 \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief] [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 [Content Brief]
Supplier Website	https://www.medchemexpress.com/PIM-447-dihydrochloride.html
Last Update	2025-05-21 16:50:25

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