Apatorsen
Based on 2 publication(s) in Google Scholar
Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen 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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.54%
- CAS 番号: 1002331-21-6
- 分子量:7157.00
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Apatorsen
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生物活性
Apatorsen (50 nM; 2 days transfection, 48 h erlotinib co-treatment) synergistically enhances erlotinib-induced reduction in cell viability and apoptosis in A549 and HCC827 non-small cell lung cancer cells[1].
Apatorsen (12.5-100 nM (pemetrexed co-treatment); 50 nM (cisplatin, paclitaxel, gemcitabine co-treatment); 2 days treatment, 72 h chemotherapeutic co-incubation) synergistically enhances the cell viability-reducing and pro-apoptotic effects of pemetrexed, cisplatin, paclitaxel, and gemcitabine in A549 non-small cell lung cancer cells[1].
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.
化学情報
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CAS 番号 1002331-21-6
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性状 Solid
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分子量 7157.00
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Color White to off-white
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SMILES
[Apatorsen]
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別名
OGX-427
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配列
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)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°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
溶剤 & 溶解度
H2O : ≥ 20 mg/mL (2.79 mM)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 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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取扱説明書 (2242 KB)
参考文献
[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]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.1397 mL | 0.6986 mL | 1.3972 mL | 3.4931 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Apatorsen 関連分類
HY-145722A 関連分類
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