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Ralimetinib (LY2228820) dimesylate
Catalog No.S1494
For research use only.
Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
CAS No. 862507-23-1
Selleck's Ralimetinib (LY2228820) dimesylate has been cited by 59 publications
Purity & Quality Control
Choose Selective p38 MAPK Inhibitors
Related Compound Libraries
Other p38 MAPK Products
Biological Activity
| Description | Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
LY2228820 inhibits p38α, as well as the level of phosphoMAPKAPK-2 (pMK2) in RAW 264.7 cells, with IC50 values of 7 nM and 34.3 nM, respectively. Furthermore, LY2228820 inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC50 of 5.2 nM. [1] In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, LY2228820 (200 nM–800 nM) significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. LY2228820 (200 nM–400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but LY2228820 alone doesn't inhibit the growth of MM.1S cells. LY2228820 (200 nM–800 nM) also inhibits secretion of IL-6 and MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138+, CD138− or PB CD14+ cells. LY2228820 (400 nM–800 nM) also blocks osteoclastogenesis from CD14+ cells. [2] |
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| Cell Data |
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| Assay |
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| In vivo | In LPS-induced mice, LY2228820 effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED50) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), LY2228820 displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED50)of 1.5 mg/kg. [1] |
Protocol (from reference)
| Kinase Assay:[1] |
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| Cell Research:[2, 3] |
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| Animal Research:[1] |
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| References |
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Solubility (25°C)
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In vitro |
Water |
100 mg/mL
warmed (163.2 mM) |
| DMSO |
4 mg/mL
warmed (6.52 mM) |
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| Ethanol |
'3 mg/mL
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In vivo |
Add solvents to the product individually and in order |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 612.74 | ||
|---|---|---|---|
| Formula | C24H29FN6.2CH4O3S |
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| CAS No. | 862507-23-1 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC(C)(C)CN1C2=C(C=CC(=N2)C3=C(N=C(N3)C(C)(C)C)C4=CC=C(C=C4)F)N=C1N.CS(=O)(=O)O.CS(=O)(=O)O | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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g
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT02860780 | Completed | Drug: prexasertib|Drug: ralimetinib | Advanced Cancer|Metastatic Cancer|Colorectal Cancer|Non-small Cell Lung Cancer | Eli Lilly and Company | August 10 2016 | Phase 1 |
| NCT02364206 | Completed | Drug: LY2228820|Drug: Temozolomide|Radiation: radiotherapy | Adult Glioblastoma | Centre Jean Perrin|National Cancer Institute France|ARC Foundation for Cancer Research | June 8 2015 | Phase 1|Phase 2 |
| NCT02322853 | Terminated | Drug: Tamoxifen|Drug: Ralimetinib (LY2228820 dimesylate) | Postmenopausal|Metastatic Breast Cancer | Centre Francois Baclesse|National Cancer Institute France|ARC Foundation for Cancer Research | January 2015 | Phase 2 |
| NCT01393990 | Completed | Drug: LY2228820|Drug: Midazolam|Drug: Tamoxifen | Advanced Cancer | Eli Lilly and Company | September 4 2008 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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