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Bexarotene

Chemical Structure : Bexarotene

CAS No.: 153559-49-0

Bexarotene (LGD1069, LGD-1069)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 348.49
Formula C24H28O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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