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LY-2228820

  • LY-2228820 (200x200px)
  • LY-2228820 (600x600px)
Price:
$169.00
Catalog #:
C5922-5
Quantity:


Product Description

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.

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