Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
分子量
352.50
Formula
C24H24D4O2
CAS 号
2182068-00-2
中文名称
贝沙罗汀 D4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[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 (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM)[1][2][3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.
体外研究 (In Vitro)
Bexarotene selectively binds and activates RXR subtypes with Kd=14±2 nM, 21±4 nM, and 29±7 nM for RXRα, RXRβ, and RXRγ subtypes[1]. Bexarotene is effective in limiting the proliferation of leukemic (HL-60) cells. Bexarotene inhibits the proliferation of HL-60 cells by 37% at 1 μM[1]. Bexarotene monotherapy of cells shows an antiproliferative effect at a high dose, and the IC50s aere 40.62±0.45 µM (PC3) and 50.20±4.10 µM (DU145)[2]. Bexarotene (20 and 40 µM) and Docetaxel (5 and 10 µM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation[2]. Bexarotene (20 and 40 µM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[2]
Cell Line:
The human PCa androgen-independent cell lines PC3 and DU145
Concentration:
5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells.
Incubation Time:
24 and 48 hours
Result:
Showed an antiproliferative effect with the IC50s were 40.62±0.45 µM (PC3) and 50.20±4.10 µM (DU145).
Cell Viability Assay[2]
Cell Line:
PC3 and DU145 cells
Concentration:
20 and 40 µM
Incubation Time:
24 or 48 hours
Result:
Decreased cyclin D1, and cyclin E2 after 24 hours treatment. Not only decreased the expression of cyclin D1 and cyclin E2 but repressed cyclin B1 and CDK1 expression after 48 hours treatment.
体内研究 (In Vivo)
Bexarotene (1 mg/kg/day) is effective in blocking the development of behavioral deficits and dopamine neuron degeneration in a rat model of Parkinson’s disease (PD) producing significantly reduced changes in both triglycerides and T4 serum[1]. Bexarotene is an effective preventive agent against lung tumor growth and progression. Bexarotene ((100 mg/kg by gavage) inhibits both tumor multiplicity and tumor volume in mice of all three genotypes (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt). Bexarotene reduces the progression of adenoma to adenocarcinoma by ∼50% in both p53wt/wtK-rasko/wt and p53wt/wtK-raswt/wt mice[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
UL53-3 mice (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt)[3]
Dosage:
100 mg/kg
Administration:
Gavage with 18 gage of gavage-needle, 0.1 mL per mouse per day, 5 times a week, continued for 12 weeks
Result:
Inhibited both tumor multiplicity and tumor volume in mice of all three genotypes.
Clinical Trial
分子量
348.48
Formula
C24H28O2
CAS 号
153559-49-0
中文名称
贝沙罗汀;蓓萨罗丁
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Nathalia Rodrigues de Almeida, et al. A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397.
[2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886.
[3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9.