862505-00-8

862505-00-8 structure

Name: Ralimetinib
Chemical Name: 5-[2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-b]pyridin-2-amine
CAS Number: 862505-00-8
Molecular Formula: C₂₄H₂₉FN₆
Molecular Weight: 420.53
Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
Create Date: 2018-12-18 21:14:51
Modify Date: 2025-08-23 19:25:15
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].

Name	5-[2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-b]pyridin-2-amine
Synonyms	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)-

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.

862507-55-9

506-68-3

~74%

862505-00-8

Literature: ELI LILLY AND COMPANY Patent: WO2005/75478 A1, 2005 ; Location in patent: Page/Page column 49 ; WO 2005/075478 A1

862507-91-3

630-19-3

~59%

862505-00-8

Literature: ELI LILLY AND COMPANY Patent: WO2005/75478 A1, 2005 ; Location in patent: Page/Page column 55-56 ; WO 2005/075478 A1

Precursor 4
862507-55-9 506-68-3 862507-91-3 630-19-3
DownStream 0