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Ralimetinib

Names

[ CAS No. ]:
862505-00-8

[ Name ]:
Ralimetinib

[Synonym ]:
UNII-73I34XW4HD
5-[2-tert-butyl-5-(4-fluoro-phenyl)-1H-imidazol-4-yl]-3-(2,2-dimethyl-propyl)-3H-imidazo[4,5-b]pyridin-2-ylamine
Ralimetinib
3-(2,2-Dimethylpropyl)-5-[4-(4-fluorophenyl)-2-(2-methyl-2-propanyl)-1H-imidazol-5-yl]-3H-imidazo[4,5-b]pyridin-2-amine
LY2228820
5-(2-(tert-butyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-(2,2-dimethylpropyl)-3H-imidazo[4,5-b]pyridin-2-amine
3H-Imidazo[4,5-b]pyridin-2-amine, 5-[2-(1,1-dimethylethyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)-

Biological Activity

[Description]:

Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Inflammation/Immunology

[Target]

p38β MAPK:3.2 nM (IC50)

p38α MAPK:5.3 nM (IC50)


[References]

[1]. Campbell RM, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity. Mol Cancer Ther. 2014 Feb;13(2):364-74.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
634.4±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H29FN6

[ Molecular Weight ]:
420.53

[ Flash Point ]:
337.5±34.3 °C

[ Exact Mass ]:
420.243774

[ PSA ]:
86.14000

[ LogP ]:
4.94

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.631

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds