LY2228820 is a potent and selective ATP-competitive inhibitor of the α- and β-isoforms of p38 mitogen-activated protein kinases (MAPKs). It inhibits p38α and p38β with IC50 values of 5.3 nM and 3.2 nM, respectively. [1] In cell-based assays, LY2228820 selectively inhibited the level of phospho-MAPKAP-K2 (pMK2) in anisomycin-induced RAW264.7 cells, with IC50 of 35.3 nM. LY2228820 also inhibits lipopolysaccharide (LPS)/IFN-γ-induced TNFα formation in murine peritoneal macrophages, with IC50 of 6.3 nM. [1] Furthermore, LY2228820 inhibits angiogenic endothelial cord formation in multiple in vitro and in vivo assay models. [2]
LY2228820 is currently being evaluated in Phase I/II clinical trials in patients with newly diagnosed glioblastoma [3] and platinum-sensitive ovarian cancer [4]."
Technical information:
| Chemical Formula: | C24H29FN6.2CH4O3S | |
| CAS #: | 862507-23-1 | |
| Molecular Weight: | 612.74 | |
| Purity: | > 98% | |
| Appearance: | Off-white | |
| Chemical Name: | 5-(2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-neopentyl-3H-imidazo[4,5-b]pyridin-2-amine dimethanesulfonate | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | LY-2228820, LY2228820, LY2228820 dimesylate, |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Campbell RM, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity. Mol Cancer Ther. 2014; 13(2):364-74 Pubmed ID: 24356814 |
| 2. | Tate CM, et al. LY2228820 dimesylate, a selective inhibitor of p38 mitogen-activated protein kinase, reduces angiogenic endothelial cord formation in vitro and in vivo. J Biol Chem. 2013; 288(9):6743-53 Pubmed ID: 23335506 |
| 3. | Study of LY2228820 With Radiotherapy Plus Concomitant TMZ in the Treatment of Newly Diagnosed Glioblastoma (GLYRad). clinicaltrials.gov/NCT02364206 |
| 4. | A Study of LY2228820 for Recurrent Ovarian Cancer. clinicaltrials.gov/NCT01663857 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
