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Ralimetinib dimesylate

Catalog No. T6047   CAS 862507-23-1
Synonyms: LY2228820 dimesylate, Ralimetinib, LY2228820, Ralimetinib Mesylate

Ralimetinib dimesylate (LY2228820 dimesylate) is the dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Ralimetinib dimesylate Chemical Structure
Ralimetinib dimesylate, CAS 862507-23-1
Pack Size Availability Price/USD Quantity
2 mg In stock $ 54.00
5 mg In stock $ 77.00
10 mg In stock $ 134.00
25 mg In stock $ 262.00
50 mg In stock $ 474.00
100 mg In stock $ 522.00
1 mL * 10 mM (in DMSO) In stock $ 101.00
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Purity: 99.38%
Purity: 98.59%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ralimetinib dimesylate (LY2228820 dimesylate) is the dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities.
Targets&IC50 p38α:7 nM
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]
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]
Kinase Assay Inhibition of p38α: Inhibition of p38α is determined using recombinant human p38α in a standard filter binding protocol using ATP[γ-33P] and EGFR 21-mer peptide as substrate. Functional inhibition of TNFα in murine peritoneal macrophages is determined using LPS stimulation in the presence of LY2228820. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with LY2228820 and then stimulated with anisomycin. The level of p38α activity is detected using a phosphoMAPKAPK-2 (pMK2) (Thr 334) antibody which reacts with a residue specifically phosphorylated by p38α.
Cell Research MTT assays and APO 2.7 staining are performed to assess cellular proliferation and induction of apoptosis, respectively. Viability is expressed as percent viable cells. Apoptosis in cells is evaluated by APO 2.7 staining. For detection of mitochondrial membrane protein 7A6 expressed in apoptotic cells, cells are incubated with APO 2.7 reagent for 20 min. Expression of APO 2.7 is determined using an EPICS XL flow cytometer.(Only for Reference)
Synonyms LY2228820 dimesylate, Ralimetinib, LY2228820, Ralimetinib Mesylate
Molecular Weight 612.74
Formula C24H29FN6·2CH4O3S
CAS No. 862507-23-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL (44.88 mM)

TargetMolReferences and Literature

1. Mader M, et al. Bioorg Med Chem Lett, 2008, 18(1), 179-183. 2. Ishitsuka K, et al. Br J Haematol, 2008, 141(5), 598-606. 3. Ishitsuka K, et al. Oncogene, 2005, 24(38), 5888-5896. 4. Dong W, Xie W, Liu Y, et al. Receptor tyrosine kinase inhibitors block proliferation of TGEV mainly through p38 mitogen-activated protein kinase pathways[J]. Antiviral Research. 2020, 173: 104651. 5. Chiang C, Zhang M, Wang D, et al. Therapeutic potential of targeting MKK3-p38 axis with Capsaicin for Nasopharyngeal Carcinoma[J]. Theranostics. 2020, 10(17): 7906.

TargetMolCitations

1. Chiang C, Zhang M, Wang D, et al. Therapeutic potential of targeting MKK3-p38 axis with Capsaicin for Nasopharyngeal Carcinoma. Theranostics. 2020, 10(17): 7906. 2. Dong W, Xie W, Liu Y, et al. Receptor tyrosine kinase inhibitors block proliferation of TGEV mainly through p38 mitogen-activated protein kinase pathways. Antiviral Research. 2020, 173: 104651

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Aging Compound Library Anti-Cancer Compound Library HIF-1 Signaling Pathway Compound Library Apoptosis Compound Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library MAPK Inhibitor Library

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Keywords

Ralimetinib dimesylate 862507-23-1 Apoptosis Autophagy MAPK p38 MAPK Ralimetinib Dimesylate LY 2228820 Dimesylate LY2228820 Dimesylate LY-2228820 Dimesylate LY 2228820 Inhibitor LY-2228820 LY2228820 dimesylate inhibit Ralimetinib LY2228820 Ralimetinib Mesylate inhibitor

 

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