Bexarotene

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bexarotene 是一种对类视黄醇 X 受体具有特异性选择性的类视黄醇，用作治疗皮肤 T 细胞淋巴瘤的口服抗肿瘤剂。

Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.(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. 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. 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). Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation.Bexarotene (20 and 40 μM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells. (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. 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.

Cell Proliferation Assay Cell Line:The human PCa androgen-independent cell lines PC3 and DU145Concentration:5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells.Incubation Time:24 and 48?hoursResult:Showed an antiproliferative effect with the IC50s were 40.62±0.45?μM (PC3) and 50.20±4.10?μM (DU145).?Cell Viability AssayCell Line:PC3 and DU145 cellsConcentration:20 and 40?μMIncubation 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.

Animal Model:UL53-3 mice (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt)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.

LG 100069 | LGD 1069 | Ro 26-4455 | SR 11247

Metabolic Enzyme/Protease

Retinoid Receptor

RXR

Cancer

——

153559-49-0

348

C24H28O2

>98% (HPLC)

DMSO: 8 mg/mL (22.98 mM)

O=C(O)C1=CC=C(C(C2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2)=C)C=C1

4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid

(-20℃)

With Ice Pack

≥ 2 years