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| ln Vitro |
MSU-42011 (0-1 μM) has an IC50 value of 158 nM and suppresses iNOS in RAW264.7 macrophage-like cells [1]. In HepG2 cells, MSU-42011 (300 nM; 8 h) exhibits a modest induction of SREBP [1]. In HepG2 cells, MSU-42011 (0-5000 nM; 24 h) activates RXRα [1].
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| ln Vivo |
In the A/J mouse lung cancer model, MSU-42011 (25 mg/kg, PO) dramatically decreased the number, size, and overall burden of tumors. This effect lasted for 12 weeks. Less cells were actively proliferating and the amount of p-ERK was significantly lower than in the control group [1]. Combining MSU-42011 (25 mg/kg; oral; single dosage) with C/P in the A/J mouse lung cancer model resulted in the greatest reduction in tumor number, tumor size, and overall tumor burden. less macrophages in the lungs and more CD8+ T cell activation markers [1]. MSU42011 (PO; single dosage; 100 mg/kg) decreases tumor burden in a lung tumor model in mice [2].
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| Cell Assay |
RT-PCR[1]
Cell Types: HepG2 liver cancer cells Tested Concentrations: 300 nM Incubation Duration: 8 h Experimental Results: SREBP expression ranged from no change to a 1.49-fold induction compared to the vehicle control |
| Animal Protocol |
Animal/Disease Models: A/J mice (intraperitoneal (ip)injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[1]
Doses: 25 mg/ kg Route of Administration: Oral administration; One week after, ip every other week for a total of 6 injections with Carboplatin (HY-17393) (50 mg/kg) and paclitaxel (15 mg/kg); for 12 weeks Experimental Results: 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). Animal/Disease Models: A/J lung cancer model (intraperitoneal (ip)injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[2] Doses: 100 mg/kg Route of Administration: Oral administration; After 2 weeks, each mouse was intraperitoneally (ip) injected with anti-PD1 and anti-PDL1 antibodies at a rate of 50 μg/mouse, twice a week for a total of 22 times Experimental Results: demonstrated that an increase in the ratio of anti-tumor CD8 T cells to CD4, |
| 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. |
| Molecular Formula |
C24H34N2O2
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|---|---|
| Molecular Weight |
382.54
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| CAS # |
2456434-36-7
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~326.76 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6141 mL | 13.0705 mL | 26.1411 mL | |
| 5 mM | 0.5228 mL | 2.6141 mL | 5.2282 mL | |
| 10 mM | 0.2614 mL | 1.3071 mL | 2.6141 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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