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.
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- Pureté : 99.64%
- CAS No.: 2456434-36-7
- Formule: C24H34N2O2
- Masse moléculaire:382.54
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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All-trans-retinalVitamin A Metabolite -
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Retinoic acid (Standard)
Activité biologique
Description
In Vitro
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. Further protocols information, click here.
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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
In Vivo
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.
Chemical Information
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CAS No. 2456434-36-7
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Appearance Solid
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Masse moléculaire 382.54
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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 |
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