| Identification | Back Directory | [Name]
3-Pyridinecarboxylic acid, 6-[[3,5-bis(1,1-dimethylethyl)phenyl](2-methylpropyl)amino]- | [CAS]
2456434-36-7 | [Synonyms]
MSU-42011
3-Pyridinecarboxylic acid, 6-[[3,5-bis(1,1-dimethylethyl)phenyl](2-methylpropyl)amino]- | [Molecular Formula]
C24H34N2O2 | [MOL File]
2456434-36-7.mol | [Molecular Weight]
382.54 |
| Chemical Properties | Back Directory | [Boiling point ]
519.5±50.0 °C(Predicted) | [density ]
1.053±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
2.78±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 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].
| 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).
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| 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. |
| [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. DOI:10.1038/s41598-020-79260-8
[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. DOI:10.3390/cancers13195004 |
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| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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