862507-23-1
Ralimetinib dimesylate
CAS: 862507-23-1
Molecular Formula: C26H37FN6O6S2
862507-23-1 - Names and Identifiers
862507-23-1 - Physico-chemical Properties
| Molecular Formula | C26H37FN6O6S2 |
| Molar Mass | 612.7369832 |
| Solubility | Soluble in DMSO |
| Storage Condition | -20℃ |
| Use | Ralimetinib, also known as LY2228820, is a potent and selective, ATP-competitive inhibitor of the α- and β-isoforms of p38 MAPK in vitro (IC(50) = 5.3 and 3.2 nmol/L, respectively). In cell-based assays, LY2228820 potently and selectively inhibited phosphorylation of MK2 (Thr334) in anisomycin-stimulated HeLa cells (at 9.8 nmol/L by Western blot analysis) and anisomycin-induced mouse RAW264.7 macrophages (IC(50) = 35.3 nmol/L) with no changes in phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc ≤ 10 μmol/L. LY2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications. |
| Target | p38β MAPK；p38α MAPK |
| In vitro study | LY2228820 acts on RAW 264.7 cells, inhibiting p38α, and phosphate MAPKAPK-2(pMK2) levels with an IC50 of 7 nM and 34.3 nM, respectively. Moreover, LY2228820 inhibited lipopolysaccharide (LPS)-induced TNFα formation in mouse peritoneal macrophages with an IC50 of 5.2 nM. 200 nM-800 nM LY2228820 acts on multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, and significantly inhibits p38MAPK signaling by inhibiting HSP27 phosphorylation, which is a downstream target of p38MAPK, the expression level of HSP27 was not affected. 200 nM-400 nM LY2228820 enhanced Bortezomib-induced cytotoxicity and apoptosis, but LY2228820 alone did not inhibit MM.1S cell growth. 200 nM-800 nM LY2228820 acts on long-term bone marrow stromal stem cells (LT-BMSCs), bone marrow mononuclear cells (BMMNCs), peripheral blood (PB)CD138 |
| In vivo study | LY2228820 effectively inhibited TNFα formation in LPS-induced mice with a median effective dose threshold (TMED 50) of less than 1 mg/kg. LY2228820 acts in a rat model of collagen-induced arthritis (CIA) and is effective in foot swelling, bone erosion, and cartilage destruction, with a median effective dose threshold (TMED 50) of 1.5 mg/kg. |
862507-23-1 - Reference
| Reference Show more | 1: Correction: A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients with Advanced Cancer. Clin Cancer Res. 2016 May 15;22(10):2596. doi: 10.1158/1078-0432.CCR-16-0645. PubMed PMID: 27179115. 2: Browne AJ, Göbel A, Thiele S, Hofbauer LC, Rauner M, Rachner TD. p38 MAPK regulates the Wnt inhibitor Dickkopf-1 in osteotropic prostate cancer cells. Cell Death Dis. 2016 Feb 25;7:e2119. doi: 10.1038/cddis.2016.32. PubMed PMID: 26913608; PubMed Central PMCID: PMC4849158. 3: Patnaik A, Haluska P, Tolcher AW, Erlichman C, Papadopoulos KP, Lensing JL, Beeram M, Molina JR, Rasco DW, Arcos RR, Kelly CS, Wijayawardana SR, Zhang X, Stancato LF, Bell R, Shi P, Kulanthaivel P, Pitou C, Mulle LB, Farrington DL, Chan EM, Goetz MP. A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients with Advanced Cancer. Clin Cancer Res. 2016 Mar 1;22(5):1095-102. doi: 10.1158/1078-0432.CCR-15-1718. Epub 2015 Nov 18. PubMed PMID: 26581242. 4: Rachner TD, Göbel A, Browne A, Hötzel J, Rauner M, Hofbauer LC. P38 regulates the Wnt inhibitor Dickkopf-1 in breast cancer. Biochem Biophys Res Commun. 2015 Oct 30;466(4):728-32. doi: 10.1016/j.bbrc.2015.09.101. Epub 2015 Sep 25. PubMed PMID: 26407843. |
862507-23-1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.632 ml | 8.16 ml | 16.32 ml |
| 5 mM | 0.326 ml | 1.632 ml | 3.264 ml |
| 10 mM | 0.163 ml | 0.816 ml | 1.632 ml |
| 5 mM | 0.033 ml | 0.163 ml | 0.326 ml |
Last Update：2024-01-02 23:10:35
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