PIM447

Modify Date: 2024-01-20 09:51:35

PIM447 Structure
PIM447 structure
Common Name PIM447
CAS Number 1210608-43-7 Molecular Weight 440.461
Density 1.3±0.1 g/cm3 Boiling Point 493.7±45.0 °C at 760 mmHg
Molecular Formula C24H23F3N4O Melting Point N/A
MSDS N/A Flash Point 252.4±28.7 °C

 Use of PIM447


PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.target: pan-PIM inhibitor [2] [3]In vitro: PIM447 is cytotoxic for myeloma cells due to cell cycle disruption and induction of apoptosis mediated by a decrease in phospho-Bad (Ser112) and c-Myc levels and the inhibition of mTORC1 pathway. PIM447 also inhibits in vitro osteoclast formation and resorption, downregulates key molecules involved in these processes and partially disrupts the F-actin ring, while increasing osteoblast activity and mineralization.[1]In vivo: PIM447 significantly reduces the tumor burden and preventes tumor-associated bone loss in a disseminated murine model of human myeloma.[1]

 Names

Name PIM447
Synonym More Synonyms

 PIM447 Biological Activity

Description PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.target: pan-PIM inhibitor [2] [3]In vitro: PIM447 is cytotoxic for myeloma cells due to cell cycle disruption and induction of apoptosis mediated by a decrease in phospho-Bad (Ser112) and c-Myc levels and the inhibition of mTORC1 pathway. PIM447 also inhibits in vitro osteoclast formation and resorption, downregulates key molecules involved in these processes and partially disrupts the F-actin ring, while increasing osteoblast activity and mineralization.[1]In vivo: PIM447 significantly reduces the tumor burden and preventes tumor-associated bone loss in a disseminated murine model of human myeloma.[1]
Related Catalog
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.

[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

[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

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 493.7±45.0 °C at 760 mmHg
Molecular Formula C24H23F3N4O
Molecular Weight 440.461
Flash Point 252.4±28.7 °C
Exact Mass 440.182404
LogP 5.20
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.593
Storage condition -20℃

 Synonyms

9TG5O4V25H
N-{4-[(1R,3S,5S)-3-Amino-5-methylcyclohexyl]-3-pyridinyl}-6-(2,6-difluorophenyl)-5-fluoro-2-pyridinecarboxamide
2-Pyridinecarboxamide, N-[4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoro-
N-{4-[(1r,3s,5s)-3-Amino-5-Methylcyclohexyl]pyridin-3-Yl}-6-(2,6-Difluorophenyl)-5-Fluoropyridine-2-Carboxamide
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