Apatorsen sodium
Based on 2 publication(s) in Google Scholar
Apatorsen (OGX-427) sodium is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen sodium reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen sodium is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer.
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- Pureza: 98.54%
- No. CAS: 915443-09-3
- Peso molecular:7157 (free acid)
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Apatorsen sodium
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Actividad biológica
Apatorsen sodium (50 nM; transfected for 2 days, treated with erlotinib for 48 h) synergistically enhances erlotinib-induced cell viability reduction and apoptosis in A549 and HCC827 non-small cell lung cancer cells. Apatorsen sodium (12.5-100 nM (treated with pemetrexed); 50 nM (treated with cisplatin, paclitaxel, gemcitabine); treated for 2 days, co-incubated with chemotherapy drugs for 72 h) synergistically enhances the cell viability reduction and apoptosis-promoting effects of pemetrexed, cisplatin, paclitaxel and gemcitabine in A549 non-small cell lung cancer cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, HCC827 non-small cell lung cancer cells
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Concentration:50 nM
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Incubation Time:2 days (transfection); 48 h (erlotinib co-treatment)
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Result:Reduced Hsp27 protein expression. Caused greater reduction in cell viability than single-agent treatment when combined with erlotinib. Confirmed a synergistic effect with erlotinib at ED50, ED75, and ED90 for both cell lines. Increased levels of cleaved PARP and cleaved caspase-3 when combined with erlotinib. Increased the subG0 apoptotic cell fraction as measured by flow cytometry when combined with erlotinib.
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Cell Line:A549 non-small cell lung cancer cells
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Concentration:12.5-100 nM (pemetrexed co-treatment); 50 nM (cisplatin, paclitaxel, gemcitabine co-treatment)
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Incubation Time:2 days (OGX-427 treatment); 72 h (chemotherapeutic co-incubation)
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Result:Reduced cell viability more than single-agent treatment when combined with pemetrexed. Confirmed synergistic effects with pemetrexed at ED50, ED75, and ED90. Enhanced the cell viability-reducing effects of cisplatin, paclitaxel, and gemcitabine compared to single-agent treatment. Increased levels of cleaved PARP when combined with pemetrexed, cisplatin, paclitaxel, or gemcitabine.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude mice (6-8-week-old male; non-small cell lung cancer xenograft model with A549 cells)[1]
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Dosage:15 mg/kg
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Administration:i.p.; once daily for 7 days, then three times per week; 7 weeks
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Result:Reduced tumor Hsp27 protein levels.
Significantly reduced A549 xenograft growth rates when combined with erlotinib compared to scrambled control plus diluent, scrambled control plus erlotinib, and OGX-427 plus diluent.
Increased average number of TUNEL-positive apoptotic cells when combined with erlotinib compared to control groups.
Chemical Information
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No. CAS 915443-09-3
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Appearance Solid
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Peso molecular 7157 (free acid)
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Color Off-white to light yellow
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SMILES
[Apatorsen (sodium)]
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Synonyms
OGX-427 sodium
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Sequence
DNA, d(P-thio)([2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]rA-m5C-G-m5C-G-G-m5C-G-m5C-T-m5C-G-G-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]m5rU), nonadecasodium salt
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Biomolecules
Phenoxazine Derivative ST61 Displays an Oxidative-Stress-Mediated Cytotoxic Activity Against Human Cancer Cells. [Abstract]2026 May 6;16(5):689. PMID: 42194038 -
Mol Neurobiol
Identification of Axonal Regeneration-Related Genes and a Potential Analgesic Drug for Neuropathic Pain. [Abstract]2025 Nov 22;63(1):138. PMID: 41273615
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2242 KB)
Referencias
[1]. Barbara Lelj-Garolla, et al. Hsp27 inhibition with OGX-427 sensitizes non-small cell lung cancer cells to erlotinib and chemotherapy. Mol Cancer Ther. 2015 May;14(5):1107-16. [Content Brief]
[2]. Chi KN, et al. A phase I dose-escalation study of apatorsen (OGX-427), an antisense inhibitor targeting heat shock protein 27 (Hsp27), in patients with castration-resistant prostate cancer and other advanced cancers. Ann Oncol. 2016;27(6):1116-1122. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Apatorsen sodium Related Classifications
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