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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-RAR/RXR-Bexarotene
Bexarotene

Chemical Structure : Bexarotene

CAS No.: 153559-49-0

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Bexarotene (LGD1069, LGD-1069)

货号: PC-20769Not For Human Use, Lab Use Only.

Bexarotene (LGD1069) is a highly potent and selective retinoid X receptors (RXR) agonist with EC50 of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ respectively, with no affinity for RAR receptors.

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200 mg ￥1580 In stock
500 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Bexarotene (LGD1069) is a highly potent and selective retinoid X receptors (RXR) agonist with EC50 of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ respectively, with no affinity for RAR receptors.
Bexarotene (LGD1069) selectively binds and activates RXR subtypes with Kd=14 nM, 21 nM, and 29 nM for RXRα, RXRβ, and RXRγ receptors.
Bexarotene (LGD1069) activates both RXR/RXR homodimers and RAR/RXR heterodimers, could inhibit clonal growth and induce differentiation of HL-60 cells as well as leukemic cells from patients.
The combination of ATRA and LGD1069 showed synergistic effects in inducing differentiation of HL-60 cells.
Bexarotene (LGD1069) can act as a highly effective and benign chemopreventive agent for mammary carcinoma.

物理化学性质&存储条件

分子量 348.49
分子式 C24H28O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Nathalia Rodrigues de Almeida, et al. Med Res Rev. 2019 Jul;39(4):1372-1397.

2. Boehm MF, et al. J Med Chem. 1994 Sep 2;37(18):2930-41.

3. Boehm MF, et al. J Med Chem. 1995 Aug 4;38(16):3146-55.

4. Kizaki M, et al. Blood. 1996 Mar 1;87(5):1977-84.

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