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
- Molecular Weight:
- 440.4608296
- MDL Number:
- MFCD30489747
- MOL File:
- 1820565-69-2.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| PIM447 (hydrochloride) | 29718 | 1mg | $107 |
| PIM447 (hydrochloride) | 29718 | 5mg | $509 |
| PIM-447 dihydrochloride | VXC56569 | 5mg | $1008.65 |
| PIM-447 dihydrochloride | VXC56569 | 10mg | $1403.3 |
| PIM-447 dihydrochloride | VXC56569 | 25mg | $2631 |
N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide price More Price(28)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 29718 | PIM447 (hydrochloride) | 1820565-69-2 | 1mg | $107 | 2022-04-27 | Buy |
| Cayman Chemical | 29718 | PIM447 (hydrochloride) | 1820565-69-2 | 5mg | $509 | 2022-04-27 | Buy |
| Biosynth | VXC56569 | PIM-447 dihydrochloride | 1820565-69-2 | 5mg | $1008.65 | 2026-06-05 | Buy |
| Biosynth | VXC56569 | PIM-447 dihydrochloride | 1820565-69-2 | 10mg | $1403.3 | 2026-06-05 | Buy |
| Biosynth | VXC56569 | PIM-447 dihydrochloride | 1820565-69-2 | 25mg | $2631 | 2026-06-05 | Buy |
N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide Chemical Properties,Uses,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
N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32466 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11680 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +86-18621343501; +undefined18621343501 | product@acmec-e.com | China | 33324 | 58 |
| Jilin Chinese Academy of Sciences-yanshen Technology | +undefined18143011203 | info@chemextension.com | China | 42056 | 58 |
| SHANGHAI KEAN TECHNOLOGY CO., LTD. | +8613817748580 | cooperation@kean-chem.com | China | 40066 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131956 | 58 |
| Chembest Research Laboratories Limited | 021-20908456 | sales@BioChemBest.com | China | 6002 | 61 |
