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TCS PIM-1 1

Names

[ CAS No. ]:
491871-58-0

[ Name ]:
TCS PIM-1 1

[Synonym ]:
2-oxo-4-phenyl-5H-furan-3-carbonitrile
6-(5-Bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile
TCS PIM-1 1
3-cyano-4-phenyl-2(5H)-furanone
3-Cyano-4-phenyl-2(5H)-furanon
3-Cyan-4-phenyl-2(5H)-furanon
2-oxo-4-phenyl-2,5-dihydro-furan-3-carbonitrile
2-oxo-4-phenyl-2,5-dihydro-3-furancarbonitrile
3-Pyridinecarbonitrile, 6-(5-bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-
3-cyano-4-phenyl-6-(3-bromo-6-hydroxyphenyl)-2-pyridone
3-cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone
6-(5-Bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydro-3-pyridinecarbonitrile

Biological Activity

[Description]:

TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).IC50 value: 50 nM [1]Target: Pim-1TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors.

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> Pim
Research Areas >> Cancer

[References]

[1]. Cheney IW, et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.

[2]. Shen Y, et al. Pim-1 inhibitor attenuates trinitrobenzene sulphonic acid induced colitis in the mice. Clin Res Hepatol Gastroenterol. 2018 Sep;42(4):382-386.


[Related Small Molecules]

AZD1208 | PIM-447 dihydrochloride | Pim1/AKK1-IN-1 | SGI-1776 free base | CX-6258 | TP-3654 | Hispidulin | TCS-PIM-1-4a | GDC-0339 | SMI-16a | M-110 | INCB053914 phosphate | 3,3',4',5,6,7-HEXAHYDROXYFLAVONE

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
592.6±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H11BrN2O2

[ Molecular Weight ]:
367.196

[ Flash Point ]:
312.2±30.1 °C

[ Exact Mass ]:
366.000397

[ PSA ]:
77.14000

[ LogP ]:
4.60

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.728

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds