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153559-76-3
  • names:

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

  • CAS号:

    153559-76-3

    MDL Number:
  • MF(分子式): C24H29NO2 MW(分子量): 363.5
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
LG100268
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中文别名 LG100268
英文别名 LG100268; LG 100268 ; LG-100268.
CAS号 153559-76-3
SMILES O=C(C1=CC=C(C2(C3=C(C)C=C4C(C)(C)CCC(C)(C)C4=C3)CC2)N=C1)O
Inchi 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)
InchiKey SLXTWXQUEZSSTJ-UHFFFAOYSA-N
分子式 Formula C24H29NO2
分子量 Molecular Weight 363.5
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 LG100268(CAS:153559-76-3):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionLG100268 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.
Application1
Application2
Application3
警示图
危险性 Warning
危险性警示
安全声明
安全防护
备注
[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.
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