LG100268

Modify Date: 2024-01-05 17:09:28

LG100268 Structure
LG100268 structure
 Common Name LG100268
CAS Number 153559-76-3 Molecular Weight 363.49300
Density 1.115g/cm3 Boiling Point 487ºC at 760mmHg
Molecular Formula C24H29NO2 Melting Point 275-277ºC
MSDS USA Flash Point 248.3ºC

 Use of LG100268


LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].

 Names

Name 6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid
Synonym More Synonyms

 LG100268 Biological Activity

Description LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].
Related Catalog
In Vitro LG100268 (100 nM-1 μM; 24 hours) shows a downregulation of CSF3 and a 2.5-fold decrease of CXCL2 and IL-1β mRNA expression in RAW264.7 cells[3]. Cell Viability Assay[3] Cell Line: RAW264.7 cells Concentration: 100 nM-1 μM Incubation Time: 24 hours Result: Decreased LPS induced cytokine mRNA levels.
In Vivo LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) combines with C/P presents a more markedly reduced average tumor burden than LG268 or C/P alone. The combination establish a reduced lung tumors, which represents a reduction of 82% (vs. 59%-67% with the single drugs) in comparison with the controls[3]. Animal Model: A/J mice[3] Dosage: 50 mg/kg (Combines with carboplatin (50 mg/kg i.p.) starts 1 week after the LG268 treatment diet) Administration: Oral diet; once daily; 7 weeks Result: Decreased lung tumors growth significantly in mice.
References

[1]. M F Boehm, et al. Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. J Med Chem

[2]. D S Lala, et al. Activation of Specific RXR Heterodimers by an Antagonist of RXR Homodimers.Nature. 1996 Oct 3;383(6599):450-3.

[3]. Martine Cao,et al.The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice. Cancer Prev Res (Phila). 2016 Jan;9(1):105-14.

 Chemical & Physical Properties

Density 1.115g/cm3
Boiling Point 487ºC at 760mmHg
Melting Point 275-277ºC
Molecular Formula C24H29NO2
Molecular Weight 363.49300
Flash Point 248.3ºC
Exact Mass 363.22000
PSA 50.19000
LogP 5.51710
Vapour Pressure 0mmHg at 25°C
Index of Refraction 1.577
Storage condition -20°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
US5921500
CHEMICAL NAME :
3-Pyridinecarboxylic acid, 6-(1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naph thalenyl) cyclopropyl)-
CAS REGISTRY NUMBER :
153559-76-3
LAST UPDATED :
199806
DATA ITEMS CITED :
1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
21780 ug/kg/3D-I
TOXIC EFFECTS :
Liver - other changes Biochemical - Effect on specific coenzyme - CoA
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 33,264,1996

 Safety Information

RIDADR NONH for all modes of transport

 Articles5

More Articles
The active enhancer network operated by liganded RXR supports angiogenic activity in macrophages.

Genes Dev. 28(14) , 1562-77, (2014)

RXR signaling is predicted to have a major impact in macrophages, but neither the biological consequence nor the genomic basis of its ligand activation is known. Comprehensive genome-wide studies were...

Tributyltin engages multiple nuclear receptor pathways and suppresses osteogenesis in bone marrow multipotent stromal cells.

Chem. Res. Toxicol. 28 , 1156-66, (2015)

Organotins are members of the environmental obesogen class of contaminants because they activate peroxisome proliferator-activated receptor γ (PPARγ), the essential regulator of adipogenesis. Exposure...

Research resource: transcriptome profiling of genes regulated by RXR and its permissive and nonpermissive partners in differentiating monocyte-derived dendritic cells.

Mol. Endocrinol. 24 , 2218-2231, (2010)

Retinoid X receptors (RXRs) are heterodimerization partners for many nuclear receptors and also act as homodimers. Heterodimers formed by RXR and a nonpermissive partner, e.g. retinoic acid receptor (...

 Synonyms

AmbkkkkK580
BIDD:PXR0022
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