| Identification | Back Directory | [Name]
3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone | [CAS]
491871-58-0 | [Synonyms]
CS-1482
TCS PIM-1
SC 204330
TCS PIM-1 1
TCS PIM-1 1, >=98%
SC 204330; TCS PIM 1-1
TCS PIM-1 1(sc-204330)
3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone
6-(5-Bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-3-pyridinecarbonitrile
3-Pyridinecarbonitrile, 6-(5-bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl- | [Molecular Formula]
C18H11BrN2O2 | [MDL Number]
MFCD00276275 | [MOL File]
491871-58-0.mol | [Molecular Weight]
367.2 |
| Chemical Properties | Back Directory | [Boiling point ]
592.6±50.0 °C(Predicted) | [density ]
1.63±0.1 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥12.8 mg/mL in DMSO | [form ]
solid | [pka]
6.93±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TCS PIM-1 1 is a Pim-1 kinase inhibitor. | [Definition]
ChEBI: 3-cyano-4-phenyl-6-(3-bromo-6-hydroxyphenyl)-2-pyridone is a member of the class of pyridones that is 2-pyridone carrying cyano, phenyl and 3-bromo-6-hydroxyphenyl substituents at positions 3, 4 and 6 respectively It is a pyridone, a bromophenol and a nitrile. | [Biological Activity]
tcs pim-1 1 is a selective inhibitor of pim-1 with ic50 value of 50 nm [1].pim-1 is a proto-oncogene serine/threonine-protein kinase and plays an important role in cell cycle progression, apoptosis, transcriptional activation and more general signal transduction pathways. it has been shown that pim-1 over-expression is correlated with a variety of human cancers [2].tcs pim-1 1 is a potent pim-1 inhibitor and has a better selectivity to pim-1 than to pim-2. it was revealed that tcs pim-1 1 was the most potent inhibitor of pim-1 by outlining the crystal structure and it was also shown that tcs pim-1 1 had better inhibitory activity to pim-1 compared with pim-2 [1]. | [IC 50]
PIM1: 50 nM (IC50) | [storage]
Store at +4°C | [References]
[1]. cheney, i.w., et al., identification and structure-activity relationships of substituted pyridones as inhibitors of pim-1 kinase. bioorg med chem lett, 2007. 17(6): p. 1679-83.
[2]. cen, b., et al., the pim-1 protein kinase is an important regulator of met receptor tyrosine kinase levels and signaling. mol cell biol, 2014. 34(13): p. 2517-32. |
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LETOPHARM LIMITED
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www.letopharm.com |
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SPIRO PHARMA
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www.spiropharma.com.cn |
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