LG100268 (LG268) is a potent, selective, orally bioactive retinoid X receptor (RXR) agonist with EC50s of 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. , 3 nM, 4 nM. LG100268 showed selectivity for RXR over RAR (1000-fold), with Kis of 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers and induces transcriptional activation. LG100268 may be utilized in lung cancer research.

Physicochemical Properties

Molecular Formula	C24H29NO2
Molecular Weight	363.5
Exact Mass	363.22
CAS #	153559-76-3
PubChem CID	3922
Appearance	White to off-white solid powder
Density	1.115g/cm3
Boiling Point	487ºC at 760mmHg
Melting Point	275-277ºC
Flash Point	248.3ºC
Vapour Pressure	0mmHg at 25°C
Index of Refraction	1.577
LogP	5.517
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	27
Complexity	591
Defined Atom Stereocenter Count	0
InChi Key	SLXTWXQUEZSSTJ-UHFFFAOYSA-N
InChi Code	InChI=1S/C24H29NO2/c1-15-12-18-19(23(4,5)9-8-22(18,2)3)13-17(15)24(10-11-24)20-7-6-16(14-25-20)21(26)27/h6-7,12-14H,8-11H2,1-5H3,(H,26,27)
Chemical Name	6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid
Synonyms	LG-100268.; LG 100268 ; LG100268
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In RAW264.7 cells, LG100268 (100 nM-1 μM; 24 hours) caused a 2.5-fold reduction in CXCL2 and IL-1β mRNA expression, as well as downregulation of CSF3 [3].
ln Vivo	More than either C/P or LG268 alone, LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) and C/P together decreased mean tumor burden. In comparison to the control group, the combination significantly decreased lung tumors by 82% (as opposed to 59%–67% with the single drug) [3].
Cell Assay	Cell Viability Assay[3] Cell Types: RAW264.7 Cell Tested Concentrations: 100 nM-1 μM Incubation Duration: 24 hrs (hours) Experimental Results: LPS-induced decrease in cytokine mRNA levels.
Animal Protocol	Animal/Disease Models: A/J mice [3] Doses: 50 mg/kg (in combination with carboplatin (50 mg/kg ip) starting 1 week after LG268 treatment diet) Route of Administration: Oral diet; one time/day; 7 weeks Experimental Results: Lung tumor growth in mice was Dramatically diminished.
References	[1]. Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. J Med Chem. [2]. Activation of Specific RXR Heterodimers by an Antagonist of RXR Homodimers.Nature. 1996 Oct 3;383(6599):450-3. [3]. 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.
Additional Infomation	LG-100268 is a retinoid X receptor (RXR) selective compound.

Solubility Data

Solubility (In Vitro)

DMSO : ~5.56 mg/mL (~15.30 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 0.56 mg/mL (1.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.56 mg/mL (1.54 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 0.56 mg/mL (1.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7510 mL	13.7552 mL	27.5103 mL
	5 mM	0.5502 mL	2.7510 mL	5.5021 mL
	10 mM	0.2751 mL	1.3755 mL	2.7510 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.