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MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $41 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $289 | In Stock | |
50 mg | $463 | In Stock | |
100 mg | $747 | In Stock | |
500 mg | $1,520 | In Stock |
Description | MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity. |
Targets&IC50 | iNOS:158 nM |
In vitro | MSU-42011 (300 nM; 8 h) showed a low induction effect on SREBP in HepG2 cells.[1] MSU-42011 (0-5000 nM; 24 h) can activate RXR in HepG2 cells.[1] |
In vivo | MSU-42011 (25 mg/kg; oral; for 12 weeks) significantly reduced the number, size, and overall tumor burden of tumors in the A/J mouse lung cancer model. Compared with the control group, there were fewer cells with active proliferation and showed a significant decrease in p-ERK [1]. MSU-42011 (25 mg/kg; oral; single dose) is most effective in reducing the number, size, and overall tumor burden of the A/J mouse lung cancer model in combination with C/P. Reduced macrophages in the lungs and increased activation markers of CD8+T cells [1]. MSU42011 (100 mg/kg; PO; single dose) reduces tumor burden in a mouse lung tumor model [2]. |
Molecular Weight | 382.54 |
Formula | C24H34N2O2 |
Cas No. | 2456434-36-7 |
Smiles | N(CC(C)C)(C1=CC(C(C)(C)C)=CC(C(C)(C)C)=C1)C2=CC=C(C(O)=O)C=N2 |
Relative Density. | 1.053 g/cm3 (Predicted) |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (117.63 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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