MSU-42011
Based on 1 Customer Validation
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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 : 99.64%
- CAS 番号: 2456434-36-7
- 分子式: C24H34N2O2
- 分子量:382.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Retinoic acid (Standard)
生物活性
製品説明
体外実験
MSU-42011 (0-1 μM) inhibits iNOS with an IC50 of 158 nM in RAW264.7 macrophage-like cells[1].
MSU-42011 (300 nM; 8 h) shows a low induction effect on SREBP in HepG2 cells[1].
MSU-42011 (0-5000 nM; 24 h) can activate RXRα in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 liver cancer cells
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Concentration:300 nM
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Incubation Time:8 h
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Result:SREBP expression ranged from no change to a 1.49-fold induction compared to the vehicle control
体内実験
Fewer cells actively proliferated and showed a significant [1] reduction in p-ERK compared to controls.
MSU-42011 (25 mg/kg; PO; 1 week later, intraperitoneal injection of Carboplatin (HY-17393) (50 mg/kg) and paclitaxel (HY-B0015) (15 mg/kg) every other week 6 times; treatment for 12 weeks) is most effective in reducing tumor number, tumor size, and overall tumor burden when combined with C/P in the A/J mouse lung cancer model.
Decreased macrophages in the lung and increases CD8+ T cell activation markers[1].
MSU42011 (100 mg/kg; PO; 2 weeks later, intraperitoneal injection 50mg/mouse of anti-PD1 and anti-PDL1 antibodies, twice a week, a total of 22 times) reduces tumor burden in a mouse lung tumor model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A/J mice (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[1]
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Dosage:25 mg/kg
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Administration:Oral administration; One week after, i.p. every other week for a total of 6 injections with Carboplatin (HY-17393) (50 mg/kg) and paclitaxel (15 mg/kg); for 12 weeks
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Result:The number and size of detected lung surface tumors increased not in the treatment group
Combines with C/P was most effective in reducing tumor number (67% vs. control), tumor size (76% vs. control), and overall tumor burden (92% vs. control).
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Animal Model:A/J lung cancer model (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[2]
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Dosage:100 mg/kg
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Administration:Oral administration; After 2 weeks, each mouse was intraperitoneally injected with anti-PD1 and anti-PDL1 antibodies at a rate of 50 μg/mouse, twice a week for a total of 22 times
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Result:Showed that an increase in the ratio of anti-tumor CD8 T cells to CD4, CD25 T cells resulted in a significant reduction in tumor volume compared to MSU42011 or anti-PD(L)1 antibody alone.
化学情報
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CAS 番号 2456434-36-7
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性状 Solid
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分子量 382.54
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分子式 C24H34N2O2
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Color White to off-white
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SMILES
O=C(C1=CN=C(N(CC(C)C)C2=CC(C(C)(C)C)=CC(C(C)(C)C)=C2)C=C1)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (326.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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 (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Moerland JA, et al. The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer. Sci Rep. 2020 Dec 17;10(1):22244. [Content Brief]
[2]. Ana S Leal, et al. The RXR Agonist MSU42011 Is Effective for the Treatment of Preclinical HER2+ Breast Cancer and Kras-Driven Lung Cancer. Cancers (Basel). 2021 Oct 6;13(19):5004. [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. 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 | 2.6141 mL | 13.0705 mL | 26.1411 mL | 65.3526 mL |
| 5 mM | 0.5228 mL | 2.6141 mL | 5.2282 mL | 13.0705 mL | |
| 10 mM | 0.2614 mL | 1.3071 mL | 2.6141 mL | 6.5353 mL | |
| 15 mM | 0.1743 mL | 0.8714 mL | 1.7427 mL | 4.3568 mL | |
| 20 mM | 0.1307 mL | 0.6535 mL | 1.3071 mL | 3.2676 mL | |
| 25 mM | 0.1046 mL | 0.5228 mL | 1.0456 mL | 2.6141 mL | |
| 30 mM | 0.0871 mL | 0.4357 mL | 0.8714 mL | 2.1784 mL | |
| 40 mM | 0.0654 mL | 0.3268 mL | 0.6535 mL | 1.6338 mL | |
| 50 mM | 0.0523 mL | 0.2614 mL | 0.5228 mL | 1.3071 mL | |
| 60 mM | 0.0436 mL | 0.2178 mL | 0.4357 mL | 1.0892 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8169 mL | |
| 100 mM | 0.0261 mL | 0.1307 mL | 0.2614 mL | 0.6535 mL |
MSU-42011 関連分類
HY-153832 関連分類
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