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Chemical Structure : LY2228820 dimesylate
CAS No.: 862507-23-1
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $188 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | $478 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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).
| M.Wt | 612.737 | |
| Formula | C26H37FN6O6S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: < 7.8 mg/mL |
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| 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) |
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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.
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