2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy
  4. Ralimetinib

Ralimetinib  (Synonyms: LY2228820)

製品番号: HY-13241A 純度: 98.58%
COA 取扱説明書 Technical Support

Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma.

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CAS 番号 : 862505-00-8

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カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Other Forms of Ralimetinib:

Ralimetinib 関連抗体

Top Publications Citing Use of Products

    Ralimetinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2026 Mar 5.  [Abstract]

    Spheroids were cultured for 24 h before treating with either AKTi-1/2 (5 µM) or Ralimetinib dimesylate (15 µM) for 72 h before performing Trypan Blue Exclusion Assay. Treatment with AKTi-1/2 (AKT inhibitor) and Ralimetinib dimesylate (p38 inhibitor) resulted in significantly increased cell viability in OVCAR8-ULK1KO spheroids, while no differences were observed in HEYA8-ULK1KO spheroids.

    Ralimetinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Oct 23;12(11):994.  [Abstract]

    HT-29 cells were transfected with an expression vector of flag-tagged MLKL fused with two AP20187 (10 μM)-binding (FKBPv) domains. The cells were pretreated with indicated compounds (Ralimetinib dimesylate (LY2228820, 10 μM), et al.) for 4 h followed by treatment with AP20187 to induce MLKL oligomerization. Cell viability was determined by CellTiter-Glo after treatment with AP20187 for 2 h (Left). Cell lysates were separated by non-reducing SDS/PAGE and analyzed by western blotting using MLKL antibody (Right).

    Ralimetinib purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jul;20(1):735-744.  [Abstract]

    p38 inhibitor Ralimetinib dimesylate (p38 i, 3 nM; 24 h) reduced the proinflammatory effects of Anti-22 in model in vitro. p-p38, NF-κB, COX-2 and iNOS protein expression was determined by western blotting and statistically analyzed.

    Ralimetinib purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jul;20(1):735-744.  [Abstract]

    p38 inhibitor Ralimetinib dimesylate (p38 i, 3 nM; 24 h) reduced the proinflammatory effects of Anti-22 in the in vitro stroke model. TNF-α, IL-1β, IL-6, IL-18, MIP-2 and PGE2 expression was determined by ELISA.

    Ralimetinib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2015 Nov 19;2(12):1944-56.  [Abstract]

    CRC cells were treated with 4 μM Ralimetinib dimesylate (LY2228820), 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.

    p38 MAPK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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    製品説明

    Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma[1][2].

    IC50 & Target

    p38β MAPK

    3.2 nM (IC50)

    p38α MAPK

    5.3 nM (IC50)

    体外実験

    LY2228820 (1 nmol/L-20 μmol/L; 2 h pre-incubation, 30 min anisomycin stimulation) potently inhibits p38 pathway-mediated MK2 phosphorylation in anisomycin-stimulated RAW264.7 macrophages with an IC50 of 35.3 nmol/L[1].
    LY2228820 (1 nmol/L-20 μmol/L; 0.5 h pre-incubation, 2 h LPS/IFN-γ stimulation) potently inhibits LPS/IFN-γ-induced TNF-α secretion in mouse peritoneal macrophages with an IC50 of 6.3 nmol/L[1].
    LY2228820 (9.8 nmol/L-10 μmol/L; 1 h pre-incubation, 45 min anisomycin stimulation) selectively inhibits p38 pathway-mediated MK2 phosphorylation in anisomycin-stimulated HeLa cells at 9.8 nmol/L, with no off-target effects on JNK, ERK1/2, or their downstream substrates up to 10 μmol/L[1].
    LY2228820 (1 nmol/L-20 μmol/L; 30 min pre-incubation, 72 h LPS stimulation) inhibits LPS-induced CXCL8 secretion in A549 non-small cell lung cancer cells with an IC50 of 144.9 nmol/L[1].
    LY2228820 inhibits p38 pathway-mediated MK2 phosphorylation in human peripheral blood mononuclear cells ex vivo with an IC50 of 0.12 μmol/L[1].
    Ralimetinib (1.6 μM; two 72 h treatment intervals) induces apoptosis (19.12% Annexin positivity, 14.51% sub-G1 phase) and modulates cell cycle distribution in SCC-25 cells, and enhances TGF-beta-1-induced Annexin positivity (24.23%) while causing G2/S arrest in TGF-beta-1-pretreated SCC-25 cells[2].
    Ralimetinib (1.6 μM; two 72 h treatment intervals) inhibits phosphorylation of the p38 MAPK downstream target ATF2 (Thr69/71) in SCC-25 cells, with maximal inhibition observed in TGF-beta-1-pretreated cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Ralimetinib 関連抗体

    ELISA Assay[1]

    Cell Line: Mouse RAW264.7 macrophages
    Concentration: 1 nM-20 μM
    Incubation Time: 2 h (pre-incubation); 30 min (anisomycin stimulation)
    Result: Inhibited anisomycin-induced MK2 phosphorylation with an IC50 of 35.3 nM.

    ELISA Assay[1]

    Cell Line: Mouse peritoneal macrophages
    Concentration: 1 nmol/L-20 μmol/L
    Incubation Time: 0.5 h (pre-incubation); 2 h (LPS/IFN-γ stimulation)
    Result: Reduced TNF-α secretion with an IC50 of 6.3 nmol/L.

    Western Blot Analysis[1]

    Cell Line: HeLa cells
    Concentration: 9.8 nmol/L-10 μmol/L
    Incubation Time: 1 h (pre-incubation); 45 min (anisomycin stimulation)
    Result: Inhibited phospho-Thr334-MK2 at 9.8 nmol/L. Caused complete ablation of phospho-Thr334-MK2 phosphorylation at 156 nmol/L. Showed no changes in phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc at concentrations ≤10 μmol/L.

    ELISA Assay[1]

    Cell Line: A549 non-small cell lung cancer cells
    Concentration: 1 nmol/L-20 μmol/L
    Incubation Time: 30 min (pre-incubation); 72 h (LPS stimulation)
    Result: Reduced LPS-induced CXCL8 secretion with an IC50 of 144.9 nmol/L.

    Apoptosis Analysis[2]

    Cell Line: cisplatin-resistant head and neck squamous cell carcinoma (HNSCC) SCC-25 cells
    Concentration: 1.6 μM
    Incubation Time: two 72 h treatment intervals (treatment from day 5 to day 11)
    Result: Induced Annexin positivity in 19.12% of cells. Induced 14.51% of cells in the sub-G1 (apoptotic) phase. Enhanced TGF-beta-1-induced Annexin positivity to 24.23%. Caused G2/S cell cycle arrest with increased cell population in the G2-M phase (9.77%) in TGF-beta-1-pretreated cells. Resulted in 7.88% of cells in the sub-G1 phase when combined with TGF-beta-1.

    Western Blot Analysis[2]

    Cell Line: cisplatin-resistant HNSCC SCC-25 cells
    Concentration: 1.6 μM
    Incubation Time: two 72 h treatment intervals
    Result: Reduced phosphorylated ATF2 (Thr69/71) levels compared to control. Maximally reduced phosphorylated ATF2 (Thr69/71) levels when combined with TGF-beta-1, with a statistically significant decrease relative to TGF-beta-1 treatment alone.
    Parmacokinetics
    Species Dose Route T1/2
    Mice[1] 20 mg/kg p.o. 2.8 h
    体内実験

    Ralimetinib (0.1-30 mg/kg; p.o.; single dose) dose-dependently inhibits tumor phospho-MK2 in C57BL/6 mice bearing B16-F10 melanoma, with a TED50 of 1.95 mg/kg and >40% target inhibition maintained for 4 to 8 hours after a single 10 mg/kg oral dose[1].
    Ralimetinib (20 mg/kg; p.o.; 3 times a day; continuous or intermittent schedule) administered at 20 mg/kg three times daily via continuous or intermittent oral schedules produces significant tumor growth delay in athymic nude mice bearing A549 non-small cell lung cancer xenografts[1].
    Ralimetinib (10 mg/kg; p.o.; 3 times a day; 4 days on/3 days off; 3 weeks) administered at 10 mg/kg three times daily on a 4 days on/3 days off oral schedule achieves 72% tumor growth inhibition in CD1 nu/nu mice bearing A-2780 ovarian cancer xenografts[1].
    Ralimetinib (14.7 mg/kg; p.o.; twice a day; continuous schedule) administered at 14.7 mg/kg twice daily via continuous oral schedule completely attenuates tumor growth in athymic nude mice bearing U-87MG glioma xenografts[1].
    Ralimetinib (p.o.) administered via oral schedule produces 60% tumor growth inhibition in athymic nude mice bearing MDA-MB-468 breast cancer xenografts[1].
    Ralimetinib (p.o.) administered via oral schedule produces 42% tumor growth inhibition in irradiated CB-17 SCID mice bearing OPM-2 multiple myeloma xenografts[1].
    Ralimetinib (30 mg/kg; p.o.; 3 times a day; 4 days on/3 days off; 14 consecutive days) administered at 30 mg/kg three times daily on a 4 days on/3 days off oral schedule reduces lung metastases by 57% in nude mice with B16-F10 melanoma tail vein metastases[1].
    Ralimetinib (10-30 mg/kg; p.o.; 3 times a day; 3 days on/3 days off; 3 weeks) administered at 10 mg/kg or 30 mg/kg three times daily on a 3 days on/3 days off oral schedule produces 50% to 51% tumor growth inhibition in female athymic nude mice with orthotopic intraperitoneal SK-OV-3 ovarian cancer xenografts[1].
    Ralimetinib (30 mg/kg; p.o.; 3 times a day; continuous; 3 weeks) administered at 30 mg/kg three times daily via continuous oral schedule produces a 44% decrease in tumor luminescence and 35% reduction in tumor weight in female athymic nude mice with orthotopic renal capsule 786-O renal carcinoma xenografts[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: C57BL/6 (implanted with 2 × 106 B16-F10 melanoma cells)[1]
    Dosage: 0.1-30 mg/kg (single doses)
    Administration: p.o.; single dose
    Result: Inhibited tumor phospho-MK2 (p-Thr334) in a dose-dependent manner, with a TED50 = 1.95 mg/kg and TED70 = 11.17 mg/kg.
    Maintained >40% inhibition of tumor phospho-MK2 for 4 to 8 hours (10 mg/kg dose).
    Animal Model: Athymic nude (implanted with 1 × 107 A549 cells)[1]
    Dosage: 20 mg/kg
    Administration: p.o.; 3 times a day; continuous (days 4-38); intermittent (3 days on/3 days off, starting day 16)
    Result: Produced significant tumor growth delay compared with vehicle control.
    Showed no significant difference in efficacy between continuous and intermittent schedules.
    Animal Model: CD1 nu/nu (implanted with 2 × 106 A-2780 cells)[1]
    Dosage: 10 mg/kg
    Administration: p.o.; 3 times a day; 4 days on/3 days off; 3 weeks
    Result: Achieved 72% tumor growth inhibition on the last day of study treatment.
    Animal Model: Athymic nude (implanted with 5 × 106 U-87MG cells)[1]
    Dosage: 14.7 mg/kg
    Administration: p.o.; twice a day; continuous (days 11-28)
    Result: Completely attenuated tumor growth during the treatment period.
    Animal Model: Nude (injected via tail vein with 50,000 B16-F10 melanoma cells 1 day before treatment)[1]
    Dosage: 10 mg/kg; 30 mg/kg
    Administration: p.o.; 3 times a day; 4 days on/3 days off; 14 consecutive days
    Result: Reduced the number of lung metastases by 57% at the 30 mg/kg dose.
    Animal Model: Female athymic nude (20-25 g; orthotopic implant of 2 × 106 luciferase-labeled 786-O cells into renal capsule of left kidney)[1]
    Dosage: 30 mg/kg
    Administration: p.o.; 3 times a day; continuous; 3 weeks
    Result: Produced a 44% decrease in luminescence after 3 weeks.
    Reduced average excised tumor weight by 35%.
    臨床実験
    分子量

    420.53

    分子式

    C24H29FN6
    CAS 番号
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    SMILES

    NC1=NC2=CC=C(C3=C(C4=CC=C(F)C=C4)N=C(C(C)(C)C)N3)N=C2N1CC(C)(C)C
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    保管条件
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    In solvent -80°C 6 months
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    溶剤 & 溶解度
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    DMSO : 100 mg/mL (237.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3780 mL 11.8898 mL 23.7795 mL
    5 mM 0.4756 mL 2.3780 mL 4.7559 mL
    10 mM 0.2378 mL 1.1890 mL 2.3780 mL
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    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3780 mL 11.8898 mL 23.7795 mL 59.4488 mL
    5 mM 0.4756 mL 2.3780 mL 4.7559 mL 11.8898 mL
    10 mM 0.2378 mL 1.1890 mL 2.3780 mL 5.9449 mL
    15 mM 0.1585 mL 0.7927 mL 1.5853 mL 3.9633 mL
    20 mM 0.1189 mL 0.5945 mL 1.1890 mL 2.9724 mL
    25 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3780 mL
    30 mM 0.0793 mL 0.3963 mL 0.7927 mL 1.9816 mL
    40 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
    50 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1890 mL
    60 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
    80 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7431 mL
    100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5945 mL
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    Keywords:

    Ralimetinib862505-00-8LY2228820LY 2228820LY-2228820p38 MAPKAutophagyp38β MAPKRAW264.7 macrophagesHNSCC cellsSlugTNF-αHeLa cellsp38α MAPKMK2A549 cellsATF2Inhibitorinhibitorinhibit

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