Salicylate choline
Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer.
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- CAS No.: 2016-36-6
- Formule: C12H19NO4
- Masse moléculaire:241.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
Salicylate choline (24 h) significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in HGF-1 cells[1].
Salicylate choline (2-3 mM, 48-72 h) combined with Selinexor (KPT-330) (HY-17536) exhibits potent anti-proliferative activity against hematologic malignancy cells including MCL (JeKo-1, Mino), TCL (SR-786, Karpas-299), DLBCL (OCI-Ly1, OCI-Ly3, OCI-Ly19, SU-DHL-6, RPMI), MM (U266, OPM2, Xg1, KMS2), WM (BCWM, MWCL), ALL (RPCI, CRL-1783) and solid tumor cells including pancreatic cancer (Panc-1, L3.6pl), non-small cell lung cancer (H460, A549, HCC827), small-cell lung cancer (H1048), sarcoma (FuJi, SW872), breast cancer (Hs 578T, BT-474, BT-20, MCF7)[4].
Salicylate choline (3 mM, 24 h) combined with Selinexor significantly downregulates Rad51 and thymidylate synthase (TYMS) expression and increases γ-H2AX (DNA damage marker) levels in JeKo-1 cells[4].
Salicylate choline (3 mM, 24-48 h) combined with Selinexor significantly suppresses G2/M phase-related proteins (PLK1, Bub1b, Aurora A) expression in OCI-Ly1 cells (DLBCL) after release from double-thymidine block[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-Ly1 cells
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Concentration:3 mM combined with Selinexor
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Incubation Time:24, 36, 48 h
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Result:Suppressed G2/M phase-related proteins (PLK1, Bub1b, Aurora A) expression in OCI-Ly1 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:JeKo-1 cells (5 × 106) were subcutaneously implanted into the flanks of 4-6 weeks old male NSG mice[4]
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Dosage:500 mg/kg combined with Selinexor (15 mg/kg, p.o., twice weekly, 26 days)
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Administration:p.o., consecutively 6 days per week, 26 days
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Result:Achieved significant tumor growth inhibition.
Showed no significant changes in body weight.
- Flow cytometric DNA-content cell-cycle staining
- BrdU Incorporation Assay
- Patient-Derived Xenograft (PDX)
- Protocol for Cell Cycle
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Research Protocol for Inflammation-related Diseases
- Subcutaneous Cell-Line-Derived Xenograft
- Genotoxicity/Mutagenicity Study
- Orthotopic Cell-Line Xenograft
- Pyroptosis Solutions
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 2016-36-6
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Masse moléculaire 241.28
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Formule C12H19NO4
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SMILES
O=C(O)C1=CC=CC=C1[O-].C[N+](C)(CCO)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Tiras M, et al. In vitro assessment of cytokine modulation by choline salicylate, hyaluronic acid, lidocaine-based six different teething gels in human gingival fibroblast cells. Odontology. 2025 May 13. [Content Brief]
[2]. SCULLY FJ. Choline salicylate: an effective, well-tolerated drug for treatment of rheumatic diseases. South Med J. 1960 Jan;53:12-6. [Content Brief]
[3]. Wróblewska KB, et al. Choline Salicylate Analysis: Chemical Stability and Degradation Product Identification. Molecules. 2019 Dec 22;25(1):51. [Content Brief]
[4]. Abeykoon JP, et al. Salicylates enhance CRM1 inhibitor antitumor activity by induction of S-phase arrest and impairment of DNA-damage repair. Blood. 2021 Jan 28;137(4):513-523. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Salicylate choline Related Classifications
HY-W338346 Related Classifications
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