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Bexarotene

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Chemical Structure| 153559-49-0 同义名 : 贝沙罗汀 ;LGD1069;LG 100069;US brand name: Targretin.;3-methyl TTNEB. Bexarotene;Ro 26-445;SR 11247;Ro 26-4455
CAS号 : 153559-49-0
货号 : A129004
分子式 : C24H28O2
纯度 : 98%
分子量 : 348.478
MDL号 : -
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(172.18 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Retinoid receptors are a family of intracellular hormone receptors consisting of retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Bexarotene is a selective activator of RXRs with EC50 values of 28, 25, and 20 nM for RXRa, b, and g, respectively[5]. In BEAS-2B cells, 1 µM bexarotene remarkably promoted UBE1L immunoblot expression 10 days following the treatment compared to vehicle-treated cells. Bexarotene treatment (0.05 – 0.5 µM) also dose-dependently inhibited BEAS-2B clonal growth[6]. In Sprague-Dawley rats with NMU-induced tumors, daily administration of bexarotene (p.o., 100 mg/kg) for 6 weeks significantly suppressed tumor growth compared to vehicle-treated group. Bexarotene at 100 mg/kg completed regressed 72.2% of the primary tumors and partially suppressed 16.7% of the tumors. Administration of bexarotene at 10 and 30 mg/kg also showed anti-tumor efficacy with 10.5% and 27.8%, respectively, of tumors completely regressing. Compared to vehicle-administered control rats, bexarotene-treated animals showed decreased tumor burden at a dose-dependent manner with the values of 376, 121, and 95 mm2 at 10, 30, and 100 mg/kg, respectively. Moreover, bexarotene treatment (100 mg/kg) significantly reduced cellular proliferation index in the NMU-induced rat mammary carcinoma model[7].
作用机制 Bexarotene is a synthetic high-affinity ligand for RXRs that activates the dimerization of RXR and its partner to regulate gene expression[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.43mL

28.70mL

5.74mL

2.87mL
参考文献

[1]Nieto-Rementeria N, Perez-Yarza G, et al. Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26.

[2]Zhang C, Hazarika P, et al. 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.

[3]Bexarotene treatment does not clear β-Amyloid in an AD mouse model and Beagle dogs

[4]LGD1069

[5]Boehm MF, Zhang L, Zhi L, McClurg MR, Berger E, Wagoner M, Mais DE, Suto CM, Davies JA, Heyman RA, 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.

[6]Feng Q, Sekula D, Guo Y, Liu X, Black CC, Galimberti F, Shah SJ, Sempere LF, Memoli V, Andersen JB, Hassel BA, Dragnev K, Dmitrovsky E. UBE1L causes lung cancer growth suppression by targeting cyclin D1. Mol Cancer Ther. 2008 Dec;7(12):3780-8.

[7]Bischoff ED, Gottardis MM, Moon TE, Heyman RA, Lamph WW. Beyond tamoxifen: the retinoid X receptor-selective ligand LGD1069 (TARGRETIN) causes complete regression of mammary carcinoma. Cancer Res. 1998 Feb 1;58(3):479-84.