| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H34N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
MSU-42011 is an orally active retinoid X receptor (RXR) agonist that inhibits iNOS activity and reduces expression of the p-ERK protein, and it has immunomodulatory and antitumor activity[1]. It is supplied as a white to off-white solid (C24H34N2O2, MW 382.54) at 99.64% purity.
Physical & Chemical Properties
| CAS Number | 2456434-36-7 |
|---|---|
| Molecular Formula | C24H34N2O2 |
| Molecular Weight | 382.54 g/mol |
| Purity | 99.64% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Signaling Pathway | Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor; Immunology/Inflammation |
| Solubility | In Vitro: DMSO: 125 mg/mL (326.76 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 125 mg/mL (326.76 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In RAW264.7 macrophage-like cells, MSU-42011 (0-1 μM) inhibits iNOS, with an IC50 of 158 nM[1]. In HepG2 cells, MSU-42011 (300 nM; 8 h) has a low inducing effect on SREBP[1]. In HepG2 cells, MSU-42011 (0-5000 nM; 24 h) can activate RXRα[1].
RT-PCR[1]
| Cell Line | HepG2 liver cancer cells |
|---|---|
| Concentration | 300 nM |
| Incubation Time | 8 h |
| Result | SREBP expression ranged from no change to a 1.49-fold induction compared to the vehicle control |
In Vivo
In an A/J mouse lung cancer model, MSU-42011 (25 mg/kg, PO, for 12 weeks) significantly lowers the number, size and overall tumor burden of tumors. Fewer cells were actively proliferating, and p-ERK was significantly reduced [1] relative to controls. In the A/J mouse lung cancer model, MSU-42011 (PO, 25 mg/kg; followed 1 week later by intraperitoneal injection of Carboplatin at 50 mg/kg and paclitaxel at 15 mg/kg, given 6 times every other week; 12 weeks of treatment) gives the largest reduction in tumor number, tumor size, and overall tumor burden when combined with C/P. Lung macrophages decrease and CD8+ T cell activation markers increase[1]. In a mouse lung tumor model, MSU42011 (PO, 100 mg/kg; followed 2 weeks later by intraperitoneal injection of anti-PD1 and anti-PDL1 antibodies at 50mg/mouse, twice a week, 22 times in total) reduces tumor burden[2].
| Animal Model | A/J mice (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[1] |
|---|---|
| Dosage | 25 mg/kg |
| Administration | Oral administration; One week after, i.p. every other week for a total of 6 injections with Carboplatin (50 mg/kg) and paclitaxel (15 mg/kg); for 12 weeks |
| 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). |
| Animal Model | A/J lung cancer model (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)[2] |
|---|---|
| Dosage | 100 mg/kg |
| 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 |
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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