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  3. MSU-42011

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.

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MSU-42011 Chemical Structure

MSU-42011 Chemical Structure

CAS No. : 2456434-36-7

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10 mg USD 190 In-stock
25 mg USD 350 In-stock
50 mg USD 560 In-stock
100 mg USD 900 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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.

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

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 (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.

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 (HY-17393) (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.
Molecular Weight

382.54

Formula

C24H34N2O2

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MSU-42011
Cat. No.:
HY-153832
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