MSU-42011 |
Catalog No.GC73494
One-Click Copy Product Info
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MSU-42011 es un agonista oral activo del receptor retinox (RXR).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2456434-36-7
Sample solution is provided at 25 µL, 10mM.
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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.
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].
MSU-42011 (25 mg/kg, PO, for 12 weeks) significantly reduces the number, size and overall tumor burden of tumors in an A/J mouse lung cancer model.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 (50 mg/kg) and paclitaxel (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].
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.
[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.
| Cas No. | 2456434-36-7 | SDF | |
| Formula | C24H34N2O2 | M.Wt | 382.54 |
| Solubility | DMSO : 125 mg/mL (326.76 mM; ultrasonic and warming and heat to 60°C) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6141 mL | 13.0705 mL | 26.1411 mL |
| 5 mM | 522.8 μL | 2.6141 mL | 5.2282 mL |
| 10 mM | 261.4 μL | 1.3071 mL | 2.6141 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)