Bexarotene (Synonyms: LG 100069, LGD 1069, Ro 264455, SR 11247) |
| Catalog No.GC10037 |
벡사로텐(LGD1069)은 RXRα, RXRβ 및 RXRγ에 대해 각각 33, 24, 25nM의 EC50을 갖는 고친화성 및 선택적 레티노이드 X 수용체(RXR) 작용제입니다. 벡사로텐은 RAR 수용체에 대해 제한된 친화성을 나타냅니다(EC50>10000nM). Bexarotene은 피부 T 세포 림프종의 연구에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 153559-49-0
Sample solution is provided at 25 µL, 10mM.
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Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
References:
[1]. Vakeva L, Ranki A, Hahtola S.Ten-year experience of bexarotene therapy for cutaneous T-cell lymphoma in Finland.Acta Derm Venereol. 2012 May;92(3):258-63. doi: 10.2340/00015555-1359.
[2]. Gui Y, et al. Bexarotent attenuated CCI-induced spinal neuroinflammation and neuropathic pain by targeting MKP-1. J Pain. 2019 Jan 17. pii: S1526-5900(18)30607-2.
[3]. Zhang X, Schlaak M, Fabri M, Mauch C, Kurschat P.Successful Treatment of a Panniculitis-Like Primary Cutaneous T-Cell Lymphoma of the α/β Type with Bexarotene.Case Rep Dermatol. 2012 Jan;4(1):56-60.
[4]. Orendas P, Kubatka P, Kajo K, Stollarova N, Kassayova M, Bojkova B, Pec M, Nosal V, Kiskova T, Zihlavnikova K, Karsnakova R.Melatonin enhanced bexarotene efficacy in experimental mammary carcinogenesis.Neoplasma. 2012;59(4):469-74.
[5]. Cras A, Politis B, Balitrand N, Darsin-Bettinger D, Boelle PY, Cassinat B, Toubert ME, Chomienne C.Bexarotene via CBP/p300 induces suppression of NF-κB-dependent cell growth and invasion in thyroid cancer.Clin Cancer Res. 2012 Jan 15;18(2):442-53.
| Cell experiment [1]: | |
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Cell lines |
MJ, Hut78 and HH cell lines |
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Preparation method |
The solubility of this compound in DMSO is > 10.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
0.1, 1 and 10 μM; 24, 48, 72 and 96 hrs |
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Applications |
In MJ, Hut78 and HH cell lines, Bexarotene treatment for 96 hrs dose-dependently inhibited cell growth. In addition, Bexarotene increased the number of cells in the sub-G1 phase in a dose-dependent manner, which was accompanied by a loss of cells in the G1, S, and G2-M phases. However, Bexarotene did not show significant inhibition effect on cell growth and apoptosis at the dose of 0.1 to 10 μM over the period of 24 to 72 hrs in all 3 cell lines. |
| Animal experiment [2]: | |
|
Animal models |
MMTV-erbB2 mice |
|
Dosage form |
100 mg/kg; p.o.; q.d., 6 days per week |
|
Applications |
In MMTV-erbB2 mice, Bexarotene treatment prevented the development of hyperplasias or mammary intraepithelial neoplasia (MIN) lesions. Moreover, Bexarotene significantly inhibited mammary gland proliferation after 2- and 4- month treatments. The immunohistochemical results showed that less than 1% of mammary epithelial cells in the Bexarotene treatment group showed positive caspase 3 staining, indicating that the cancer preventive effect of Bexarotene was not attributed to the induction of apoptosis. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Zhang C, Hazarika P, Ni X, Weidner DA, Duvic M. Induction of apoptosis by bexarotene in cutaneous T-cell lymphoma cells: relevance to mechanism of therapeutic action. Clin Cancer Res. 2002 May;8(5):1234-40. [2]. Li Y, Zhang Y, Hill J, Kim HT, Shen Q, Bissonnette RP, Lamph WW, Brown PH. The rexinoid, bexarotene, prevents the development of premalignant lesions in MMTV-erbB2 mice. Br J Cancer. 2008 Apr 22;98(8):1380-8. | |
| Cas No. | 153559-49-0 | SDF | |
| Synonyms | LG 100069, LGD 1069, Ro 264455, SR 11247 | ||
| Chemical Name | 4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoic acid | ||
| Canonical SMILES | CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C | ||
| Formula | C24H28O2 | M.Wt | 348 |
| Solubility | ≥ 10.35mg/mL in DMSO | 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 | 2.8736 mL | 14.3678 mL | 28.7356 mL |
| 5 mM | 0.5747 mL | 2.8736 mL | 5.7471 mL |
| 10 mM | 0.2874 mL | 1.4368 mL | 2.8736 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 ddH2O, 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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