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MedKoo Cat#: 532109 | Name: LG100268
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LG100268 is a potent and selective rexinoid and retinoid-X receptor (RXR) agonist. LG100268 binds to the α, β and γ RXR receptors with an IC50 = 3-4 nM and has no activity at the RAR retinoic acid receptors.

Chemical Structure

LG100268
LG100268
CAS#153559-76-3

Theoretical Analysis

MedKoo Cat#: 532109

Name: LG100268

CAS#: 153559-76-3

Chemical Formula: C24H29NO2

Exact Mass: 363.2198

Molecular Weight: 363.50

Elemental Analysis: C, 79.30; H, 8.04; N, 3.85; O, 8.80

Price and Availability

Size Price Availability Quantity
10mg USD 310.00 2 Weeks
25mg USD 650.00 2 Weeks
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Related CAS #
No Data
Synonym
LG100268; LG 100268 ; LG-100268.
IUPAC/Chemical Name
6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid
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)
SMILES Code
O=C(C1=CC=C(C2(C3=C(C)C=C4C(C)(C)CCC(C)(C)C4=C3)CC2)N=C1)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
Flow cytometry analysis showed that LG268 accelerated apoptosis in NB4 cells in a time- dependent manner and that LG268 treatment led to cell cycle arrest at G0/G1 phase. Moreover, LG268 significantly decreased the protein levels of Survivin, c-Myc, and cyclinD1. Reference: Int J Med Sci. 2016 Jun 29;13(7):517-23. https://pubmed.ncbi.nlm.nih.gov/27429588/
In vivo activity:
Treatment with LG 268, but not bexarotene, decreased infiltration of myeloid-derived suppressor cells and CD206-expressing macrophages, increased the expression of PD-L1 by 50%, and increased the ratio of CD8/CD4, CD25 T cells, which correlates with increased cytotoxic activity of CD8 T cells in tumors of MMTV-Neu mice (a model of HER2-positive breast cancer). In the MMTV-PyMT murine model of triple negative breast cancer, LG268 treatment of established tumors prolonged survival, and in combination with anti-PD-L1 antibodies, significantly (p = 0.05) increased the infiltration of cytotoxic CD8 T cells and apoptosis. Reference: NPJ Breast Cancer. 2019 Nov 1;5:39. https://pubmed.ncbi.nlm.nih.gov/31700995/
Solvent mg/mL mM comments
Solubility
DMF 20.0 55.02
DMSO 14.6 40.10
Ethanol 1.0 2.75
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 363.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Xu T, Zhong L, Gan LG, Xiao CL, Shan ZL, Yang R, Song H, Li L, Liu BZ. Effects of LG268 on Cell Proliferation and Apoptosis of NB4 Cells. Int J Med Sci. 2016 Jun 29;13(7):517-23. doi: 10.7150/ijms.15507. PMID: 27429588; PMCID: PMC4946122. 2. Bouchard F, Paquin J. Differential effects of retinoids and inhibitors of ERK and p38 signaling on adipogenic and myogenic differentiation of P19 stem cells. Stem Cells Dev. 2013 Jul 15;22(14):2003-16. doi: 10.1089/scd.2012.0209. Epub 2013 Apr 1. PMID: 23441952; PMCID: PMC3699902. 3. Leal AS, Zydeck K, Carapellucci S, Reich LA, Zhang D, Moerland JA, Sporn MB, Liby KT. Retinoid X receptor agonist LG100268 modulates the immune microenvironment in preclinical breast cancer models. NPJ Breast Cancer. 2019 Nov 1;5:39. doi: 10.1038/s41523-019-0135-5. PMID: 31700995; PMCID: PMC6825145. 4. Cao M, Royce DB, Risingsong R, Williams CR, Sporn MB, Liby KT. 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. doi: 10.1158/1940-6207.CAPR-15-0325. Epub 2015 Nov 10. PMID: 26554632.
In vitro protocol:
1. Xu T, Zhong L, Gan LG, Xiao CL, Shan ZL, Yang R, Song H, Li L, Liu BZ. Effects of LG268 on Cell Proliferation and Apoptosis of NB4 Cells. Int J Med Sci. 2016 Jun 29;13(7):517-23. doi: 10.7150/ijms.15507. PMID: 27429588; PMCID: PMC4946122. 2. Bouchard F, Paquin J. Differential effects of retinoids and inhibitors of ERK and p38 signaling on adipogenic and myogenic differentiation of P19 stem cells. Stem Cells Dev. 2013 Jul 15;22(14):2003-16. doi: 10.1089/scd.2012.0209. Epub 2013 Apr 1. PMID: 23441952; PMCID: PMC3699902.
In vivo protocol:
1. Leal AS, Zydeck K, Carapellucci S, Reich LA, Zhang D, Moerland JA, Sporn MB, Liby KT. Retinoid X receptor agonist LG100268 modulates the immune microenvironment in preclinical breast cancer models. NPJ Breast Cancer. 2019 Nov 1;5:39. doi: 10.1038/s41523-019-0135-5. PMID: 31700995; PMCID: PMC6825145. 2. Cao M, Royce DB, Risingsong R, Williams CR, Sporn MB, Liby KT. 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. doi: 10.1158/1940-6207.CAPR-15-0325. Epub 2015 Nov 10. PMID: 26554632.
1: Cao M, Royce DB, Risingsong R, Williams CR, Sporn MB, Liby KT. 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. doi: 10.1158/1940-6207.CAPR-15-0325. PubMed PMID: 26554632. 2: Seo HS, Woo JK, Shin YC, Ko SG. Identification of biomarkers regulated by rexinoids (LGD1069, LG100268 and Ro25-7386) in human breast cells using Affymetrix microarray. Mol Med Rep. 2015 Jul;12(1):800-18. doi: 10.3892/mmr.2015.3480. PubMed PMID: 25778982; PubMed Central PMCID: PMC4438952. 3: Mazumdar A, Medina D, Kittrell FS, Zhang Y, Hill JL, Edwards DE, Bissonnette RP, Brown PH. The combination of tamoxifen and the rexinoid LG100268 prevents ER-positive and ER-negative mammary tumors in p53-null mammary gland mice. Cancer Prev Res (Phila). 2012 Oct;5(10):1195-202. doi: 10.1158/1940-6207.CAPR-11-0524. PubMed PMID: 22926341; PubMed Central PMCID: PMC3837417. 4: Liby K, Risingsong R, Royce DB, Williams CR, Ma T, Yore MM, Sporn MB. Triterpenoids CDDO-methyl ester or CDDO-ethyl amide and rexinoids LG100268 or NRX194204 for prevention and treatment of lung cancer in mice. Cancer Prev Res (Phila). 2009 Dec;2(12):1050-8. doi: 10.1158/1940-6207.CAPR-09-0085. PubMed PMID: 19952361; PubMed Central PMCID: PMC2818234. 5: Liby K, Risingsong R, Royce DB, Williams CR, Yore MM, Honda T, Gribble GW, Lamph WW, Vannini N, Sogno I, Albini A, Sporn MB. Prevention and treatment of experimental estrogen receptor-negative mammary carcinogenesis by the synthetic triterpenoid CDDO-methyl Ester and the rexinoid LG100268. Clin Cancer Res. 2008 Jul 15;14(14):4556-63. doi: 10.1158/1078-0432.CCR-08-0040. PubMed PMID: 18628471; PubMed Central PMCID: PMC5048101. 6: Liby K, Black CC, Royce DB, Williams CR, Risingsong R, Yore MM, Liu X, Honda T, Gribble GW, Lamph WW, Sporn TA, Dmitrovsky E, Sporn MB. The rexinoid LG100268 and the synthetic triterpenoid CDDO-methyl amide are more potent than erlotinib for prevention of mouse lung carcinogenesis. Mol Cancer Ther. 2008 May;7(5):1251-7. doi: 10.1158/1535-7163.MCT-08-0023. PubMed PMID: 18483313; PubMed Central PMCID: PMC4036619. 7: Li Y, Zhang Y, Hill J, Shen Q, Kim HT, Xu X, Hilsenbeck SG, Bissonnette RP, Lamph WW, Brown PH. The Rexinoid LG100268 prevents the development of preinvasive and invasive estrogen receptor negative tumors in MMTV-erbB2 mice. Clin Cancer Res. 2007 Oct 15;13(20):6224-31. PubMed PMID: 17947490. 8: Liby K, Rendi M, Suh N, Royce DB, Risingsong R, Williams CR, Lamph W, Labrie F, Krajewski S, Xu X, Kim H, Brown P, Sporn MB. The combination of the rexinoid, LG100268, and a selective estrogen receptor modulator, either arzoxifene or acolbifene, synergizes in the prevention and treatment of mammary tumors in an estrogen receptor-negative model of breast cancer. Clin Cancer Res. 2006 Oct 1;12(19):5902-9. PubMed PMID: 17020999. 9: Rendi MH, Suh N, Lamph WW, Krajewski S, Reed JC, Heyman RA, Berchuck A, Liby K, Risingsong R, Royce DB, Williams CR, Sporn MB. The selective estrogen receptor modulator arzoxifene and the rexinoid LG100268 cooperate to promote transforming growth factor beta-dependent apoptosis in breast cancer. Cancer Res. 2004 May 15;64(10):3566-71. PubMed PMID: 15150113. 10: Lenhard JM, Lancaster ME, Paulik MA, Weiel JE, Binz JG, Sundseth SS, Gaskill BA, Lightfoot RM, Brown HR. The RXR agonist LG100268 causes hepatomegaly, improves glycaemic control and decreases cardiovascular risk and cachexia in diabetic mice suffering from pancreatic beta-cell dysfunction. Diabetologia. 1999 May;42(5):545-54. PubMed PMID: 10333046.