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Bexarotene
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bexarotene图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议

产品介绍
Bexarotene (LGD1069) 是一种高亲和力和选择性的类视黄醇 X 受体 (RXR) 激动剂,对 RXRα、RXRβ 和 RXRγ 的 EC50 分别为 33、24、25 nM。 Bexarotene 对 RAR 受体的亲和力有限 (EC50 >10000 nM)。贝沙罗汀可用于皮肤T细胞淋巴瘤的研究。

Cell lines

MJ, Hut78 and HH cell lines

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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

0.1, 1 and 10 μM; 24, 48, 72 and 96 hrs

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 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.

产品描述

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.