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.
For research use only. We do not sell to patients.
- Purity : 99.64%
- CAS No.: 2456434-36-7
- Formula: C24H34N2O2
- Molecular Weight:382.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Retinoic acid (Standard)
Biological Activity
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.
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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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Molecular Weight 382.54
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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
| 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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