LG 100268 (Synonyms: AGN 192620, CD3127) |
Katalog-Nr.GC44059
One-Click Copy Product Info
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LG 100268 (LG268) ist ein potenter, selektiver und oral aktiver Retinoid-X-Rezeptor (RXR)-Agonist mit EC50-Werten von 4 nM, 3 nM und 4 nM für RXR-α, RXR-β bzw. RXR-γ.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 153559-76-3
Sample solution is provided at 25 µL, 10mM.
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LG 100268 is a highly potent and selective retinoid X receptor (RXR) agonist which strongly activates RXR homodimers with EC50 value of 4nM[1].
In vitro, LG 100268 (0.1-10µM) treatment on human normal mammary epithelial cells for 10 days significantly suppressed cell growth at 10µM, uprelgated the expression of pro-apoptotic BAX and E-cadherin and repressed the expression of cell division cycle 42 (CDC42) and collagen type VI α3[2]. LG 100268 (1μM) incubation on human leukemia cells (HL-60 cells) for 72h significantly elevated tissue transglutaminase (TGase) activity without inducing apoptosis[3]. LG 100268 (1μM) incubated mouse meibomian gland epithelial cells for three days after latanoprost pre-treatment. LG 100268 exerted anti-inflammatory effect by significantly suppressing IL-6 secretion induced by latanoprost and down-regulating the expression of hyperkeratinization marker Keratin-17[4].
In vivo, LG 100268 (10mg/kg or 100mg/kg) was administrated into MMTV-erbB2 transgenic mice daily with gastric gavage for 4 months or a long term of 18 months. Short-term treatment of LG 100268 significantly prevented the development of preinvasive mammary lesions including hyperplasia and ductal carcinoma in situ. Long-term treatment with LG 100268 significantly prevented invasive mammary tumor development[5]. LG 100268 (100mg/kg) was fed to MMTV-Neu mice of breast cancer for 5 days. LG 100268 reduced tumor burden, down-regulated the tumor-promoting macrophage marker CD206 and increased the percentage of naive and central memory CD8 T cells[6]. LG 100268 (100mg/kg or 40mg/kg) was fed to vinyl carbamate induced lung cancer mice model for 16 weeks. LG 100268 reduced tumor number, shrinked average tumor size and altered lipid levels by decreasing plasma triglycerides levels and free glycerol content[7].
References:
[1] Lala D S, Mukherjee R, Schulman G, et al. Activation of specific RXR heterodimers by an antagonist of RXR homodimers. Nature. 1996 Oct 3;383(6599):450-3.
[2] Seo H S, Woo J K, Shin Y C, Ko S G. 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.
[3] Boehm M F, Zhang L, Zhi L, et al. Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells. J Med Chem. 1995 Aug 4;38(16):3146-55.
[4] Jiang X Y, Yang P S, Xiao O, et al. Effects of PPAR-γ and RXR-α on mouse meibomian gland epithelial cells during inflammation induced by latanoprost. Exp Eye Res.2022 Nov:224:109251.
[5] Li Y X, Zhang Y, Hill J, et al. 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.
[6] Leal A S, Zydeck K, Carapellucci S,et al. Retinoid X receptor agonist LG100268 modulates the immune microenvironment in preclinical breast cancer models. NPJ Breast Cancer. 2019 Nov 1:5:39.
[7] Cao M, Royce D B, Risingsong R,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.
| Cell experiment [1]: | |
Cell lines | Mouse meibomian gland epithelial cells |
Preparation Method | Mouse meibomian gland epithelial cells were treated with latanoprost in the absence or presence of 1μM LG 100268 for three days. |
Reaction Conditions | 1μM; 3 days |
Applications | LG100268 could inhibit the production of IL-6 induced by latanoprost and suppressed the expression of Keratin-17. |
| Animal experiment [2]: | |
Animal models | Female MMTV-erbB2 transgenic mice |
Preparation Method | Mice were randomized into three experimental groups and treated with sesame oil or LG 100268 (10 or 100mg/kg) for 6 days per week starting at 3 months of age for 4 months or a long term of 18 months. LG 100268 was suspended in purified sesame oil and administered by daily gastric gavage using a 20-gauge gavage needle in a volume of 0.1mL. |
Dosage form | 10 or 100mg/kg; gastric gavage; daily for 4 months or 18 months |
Applications | Short-term treatment of LG 100268 significantly prevented the development of preinvasive mammary lesions including hyperplasia and ductal carcinoma in situ. Long-term treatment with LG 100268 significantly prevented invasive mammary tumor development. |
References: | |
| Cas No. | 153559-76-3 | SDF | |
| Überlieferungen | AGN 192620, CD3127 | ||
| Canonical SMILES | CC1(C)C2=C(C=C(C)C(C3(CC3)C4=NC=C(C(O)=O)C=C4)=C2)C(C)(C)CC1 | ||
| Formula | C24H29NO2 | M.Wt | 363.5 |
| Löslichkeit | DMF: 20mg/mL,DMSO: 20mg/mL,Ethanol: 1mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.751 mL | 13.7552 mL | 27.5103 mL |
| 5 mM | 550.2 μL | 2.751 mL | 5.5021 mL |
| 10 mM | 275.1 μL | 1.3755 mL | 2.751 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)