N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide

Product Name: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
CAS No.: 1820565-69-2
Chemical Name: N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
Synonyms: EOS-62253;PIM-447 2HCl;LGH-447 dihydrochloride;PIM-447 (dihydrochloride);PIM 447 dihydrochloride,PIM447 dihydrochloride;N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide dihydrochloride
CBNumber: CB73143071
Molecular Formula: C24H23F3N4O
Formula Weight: 440.4608296
MOL File: 1820565-69-2.mol

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N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide Property

storage temp.: Store at -20°C
solubility: Water:50.0(Max Conc. mg/mL);97.39(Max Conc. mM)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 29718
Product name: PIM447 (hydrochloride)
Packaging: 1mg
Price: $107
Updated: 2022/04/27

Cayman Chemical

Product number: 29718
Product name: PIM447 (hydrochloride)
Packaging: 5mg
Price: $509
Updated: 2022/04/27

ChemScene

Product number: CS-5941
Product name: PIM-447(dihydrochloride)
Purity: 99.33%
Packaging: 10mg
Price: $630
Updated: 2021/12/16

AK Scientific

Product number: 1105EH
Product name: PIM-447dihydrochloride
Packaging: 5mg
Price: $734
Updated: 2021/12/16

ChemScene

Product number: CS-5941
Product name: PIM-447(dihydrochloride)
Purity: 99.33%
Packaging: 1mg
Price: $135
Updated: 2021/12/16

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N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide Chemical Properties,Usage,Production

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

N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide Preparation Products And Raw materials

Raw materials

Preparation Products

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N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide Suppliers

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1820565-69-2, N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamideRelated Search:

PIM-447 (dihydrochloride)

LGH-447 dihydrochloride

EOS-62253

PIM-447 2HCl

PIM 447 dihydrochloride,PIM447 dihydrochloride

N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide dihydrochloride

1820565-69-2