Ralimetinib (LY2228820) dimesylate | p38 MAPK inhibitor

Chemical Structure : LY2228820 dimesylate

CAS No.: 862507-23-1

LY2228820 dimesylate (Ralimetinib dimesylate, LY-2228820)

Catalog No.: PC-43421Not For Human Use, Lab Use Only.

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

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Biological Activity

LY2228820 dimesylate (Ralimetinib) is a potent, selective, orally available inhibitor p38 MAPK with IC50 of 5.3 and 3.2 nM for p38α and p38β, respectively.
LY2228820 dimesylate (Ralimetinib) 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.
LY2228820 dimesylate (Ralimetinib) also reduces TNF-α secretion by LPS/IFN-γ–stimulated macrophages with IC50 of 6.3 nM.
LY2228820 dimesylate (Ralimetinib) 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	612.737
Formula	C26H37FN6O6S2
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	DMSO: < 7.8 mg/mL
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)-, methanesulfonate (1:2)

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.

LY2228820 dimesylate (Ralimetinib dimesylate, LY-2228820)

Biological Activity

Physicochemical Properties

References

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