Ralimetinib (LY2228820) | p38 MAPK inhibitor

Chemical Structure : Ralimetinib

CAS No.: 862505-00-8

Ralimetinib (LY2228820, LY-2228820)

Catalog No.: PC-28600Not For Human Use, Lab Use Only.

Ralimetinib (LY2228820) is a potent, selective, orally available inhibitor p38 MAPK with IC50 of 5.3 and 3.2 nM for p38α and p38β, respectively.

Packing	Price	Stock
5 mg	$198	In stock
10 mg	$328	In stock
25 mg	$528	In stock
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Biological Activity

Ralimetinib (LY2228820) is a potent, selective, orally available inhibitor of p38 MAPK with IC50 of 5.3 and 3.2 nM for p38α and p38β, respectively.
Ralimetinib (LY2228820) potently and selectively inhibits phosphorylation of MK2 (Thr334) in anisomycin-stimulated HeLa cells and mouse RAW264.7 macrophages (IC50=35.3 nM), with no changes in phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
Ralimetinib (LY2228820) also reduces TNF-α secretion by LPS/IFN-γ–stimulated macrophages with IC50 of 6.3 nM.
Ralimetinib (LY2228820) produces significant tumor growth delay in multiple in vivo cancer models (melanoma, non-small cell lung cancer, ovarian, glioma, myeloma, breast).

Physicochemical Properties

M.Wt	420.54
Formula	C24H29FN6
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3H-Imidazo[4,5-b]pyridin-2-amine, 5-[2-(1,1-dimethylethyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)-

References

1. Tate CM, et al. J Biol Chem. 2013 Mar 1;288(9):6743-53.

2. Campbell RM, et al. Mol Cancer Ther. 2014 Feb;13(2):364-74.

3. Ishitsuka K, et al. Br J Haematol. 2008 May;141(5):598-606.

4. Patnaik A, et al. Clin Cancer Res. 2016 Mar 1;22(5):1095-102.

Ralimetinib (LY2228820, LY-2228820)

Biological Activity

Physicochemical Properties

References

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