B-2422 Bexarotene, Free Acid, >99%

Synonyms : [LGD-1069] [LG 1069] [LG100069] [SR-11247]

Related Terms : [Targretin] [Targretyn] [Targrexin]

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  • 100 mg
  • 57
  • 53
  • 44
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  • 300 mg
  • 72
  • 67
  • 56
  • 11,400
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  • 500 mg
  • 98
  • 91
  • 77
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  • 1 g
  • 147
  • 136
  • 115
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  • 2 g
  • 283
  • 263
  • 222
  • 44,700
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  • 5 g
  • 655
  • 609
  • 514
  • 103,500
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  • 10 g
  • 994
  • 925
  • 781
  • 157,100
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  • M.W. 348.48
  • C24H28O2
  • [153559-49-0]
  • M.I. 14: 1194

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 65 mg/mL; soluble in ethanol at 10 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

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  • Bexarotene (LGD-1069) is a synthetic retinoid analog with specific affinity for the retinoid X receptor and belongs to a group of compounds called rexinoids. It is an oral, noncytotoxic drug that was approved in Europe and in the U.S.A. for the treatment of refractory advanced-stage cutaneous T-cell lymphomas (CTCL). Gniadecki, R., et al. "The optimal use of bexarotene in cutaneous T-cell lymphoma." Br. J. Dermatol. 157: 433-440 (2007).
  • A mouse model of Alzheimer's disease was treated with oral administration of bexarotene, a retinoid X receptor agonist. Bexarotene treatment significantly enhanced the clearance of soluble β-amyloid (Aβ) from the brain within hours in an apolipoprotein E-dependent manner. It reduced Aβ plaque area more than 50% within just 72 hours. Bexarotene treatment also resulted in the rapid reversal of cognitive, social, and olfactory deficits and improved neural circuit function. Cramer, P.E., et al. "ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models." Science 335: 1503-1506 (2012).
  • Compared with historical results with combination chemotherapy alone, bexarotene in combination with chemotherapeutic agents has showed an encouraging median survival for patients with advanced non-small cell lung cancer. Rigas, J.R. and Dragnev, K.H. "Emerging Role of Rexinoids in Non-Small Cell Lung Cancer: Focus on Bexarotene." The Oncologist 10: 22-33 (2005).
  • The receptor-selective retinoids might be particularly useful in preventing ER-negative breast cancer. Wu, K., et al. "The retinoid X receptor-selective retinoid, LGD1069, prevents the development of estrogen receptor-negative mammary tumors in transgenic mice." Cancer Res. 62: 6376-6380 (2002).
  • Results from cell culture treatments and in vivo xenograft models suggested that bexarotene in combination with chemotherapeutic agents might play an important role in preventing and overcoming acquired drug resistance in advanced prostate cancer, breast carcinoma, and non-small cell lung cancer. Ye,n W.C. and Lamph, W.W. "A selective retinoid X receptor agonist bexarotene (LGD1069, Targretin) prevents and overcomes multidrug resistance in advanced prostate cancer." Prostate 66: 305-316 (2006). Yen, W.C. and Lamph, W.W. "The selective retinoid X receptor agonist bexarotene (LGD1069, Targretin) prevents and overcomes multidrug resistance in advanced breast carcinoma." Mol. Cancer Ther. 4: 824-834 (2005). Yen, W.C., et al. "A selective retinoid X receptor agonist bexarotene (Targretin) prevents and overcomes acquired paclitaxel (Taxol) resistance in human non-small cell lung cancer." Clin. Cancer Res. 10: 8656-8664 (2004).
  • Bexarotene is the active ingredient in the drug products sold under numerous trade names, such as those listed near the top of this page as "Related Terms".  This drug is currenly approved in at least one country for treatment of patients with CTCL.  NOTE:  THE BEXAROTENE SOLD BY LC LABORATORIES FOR RESEARCH IS NOT ANY OF THE BEXAROTENE CONTAINING DRUG PRODUCTS SOLD UNDER VARIOUS TRADE NAMES AND IS NOT FOR HUMAN USE.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.