Ralimetinib

Modify Date: 2024-01-03 16:45:19

Ralimetinib Structure
Ralimetinib structure
Common Name Ralimetinib
CAS Number 862505-00-8 Molecular Weight 420.53
Density 1.2±0.1 g/cm3 Boiling Point 634.4±65.0 °C at 760 mmHg
Molecular Formula C24H29FN6 Melting Point N/A
MSDS N/A Flash Point 337.5±34.3 °C

 Use of Ralimetinib


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].

 Names

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

 Ralimetinib 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
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

~74%

Ralimetinib Structure

Ralimetinib

CAS#:862505-00-8

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

~59%

Ralimetinib Structure

Ralimetinib

CAS#: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

 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)-
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