Bexarotene - CAS 153559-49-0
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.
Publictions citing BOC Sciences Products
  • >> More
1. Combination of photodynamic therapy and immunomodulation for skin diseases-update of clinical aspects
Xiu-Li Wang, Hong-Wei Wang, Kai-Hua Yuan, Fu-Lun Li and Zheng Huang*. Photochem. Photobiol. Sci., 2011, 10, 704
Generally speaking, low-dose combination therapy may improve treatment safety and tolerability. A combination of PUVA and immune response modifier (e.g. interferon a (IFNα)-subcutaneously 3 times a week to the maximal tolerable dosage or bexarotene – orally 75–300 mg day-1) in early disease has been showntobeeffectiveandwelltolerated.IFNa and bexarotene target not only the pathogenic T-cells (e.g. direct antiproliferative effects) but can also correct the immune dysregulation in CTCL by supporting cytotoxic Th1 immune responses. In advanced stages of CTCL, extracorporeal photopheresis may be combined with IFNa or bexarotene to correct the immune dysregulation inCTCL by restoring normal equilibrium of Th1 cells. Reduced doses of these combinations, including the application of topical PDT, may also be effective as maintenance therapies following complete remission, but the durability of response and impact on overall survival remains to be determined.
2. Electron densities of bexarotene and disila-bexarotene from invariom application: a comparative study
Peter Luger,* Manuela Weber, Christian Hübschleb and Reinhold Tacke*. Org. Biomol. Chem., 2013, 11, 2348–2354
The retinoid X receptor (RXR) agonist bexarotene (1a, Targretin®) is in clinical use for the treatment of cutaneous T-cell lymphoma (Fig. 1). Recently, this agent raised additional attention in that therapeutic effects on Alzheimer’s disease in mouse models were discussed. Disila-bexarotene (1b), a silicon analogue of bexarotene (1a), was also shown to be a highly potent RXR agonist (Fig. 1), and a series of structurally related C/Si analogues were demonstrated to be very potent retinoid agonists as well. For a deeper understanding of pharmacological activities on an atomic scale, not only the geometric but also the electronic properties of the drug molecule should be examined. In the case of the C/Si analogues bexarotene (1a) and disila-bexarotene (1b), carbon and silicon differ not only in their covalent radii but also in their electronegativities. Therefore, considerable differences in the electronic properties, for example in the electrostatic potentials (ESPs), can be expected for 1a and 1b. Knowledge of these ESPs could be very helpful in characterising the pharmacological properties of these two compounds.
3. Folate-modified bexarotene-loaded bovine serum albumin nanoparticles as a promising tumor-targeting delivery system
Lisi Qi, Yuanyuan Guo, Jingjing Luan, Dianrui Zhang, Zhongxi Zhao and Yuxia Luan*. J. Mater. Chem. B,2014, 2,8361–8371
Bexarotene (BEX, also known as Targretin), (Fig. 1) a synthetic retinoid X receptor-selective activator, has been proved to be an efficacious chemopreventive and chemotherapeutic agent. As a suppressor of carcinogenesis, bexarotene can inhibit growth and induce differentiation and apoptosis in many different cancer cell lines including the prostate cancer breast cancer cell and lung cancer cell. It has been demonstrated to be extremely effective in inhibiting non-small cell lung cancer (NSCLC) and successfully used in the treatment of cutaneous T-cell lymphomas and lymphomatoid papulosis, showing promising inhibitory effects on mammary tumors and ER-negative breast cancer. Nevertheless, bexarotene is poorly water-soluble, with a maximum solubility of about 10–50 mMin pure water, resulting in poor bioavailability and limited applications. Moreover, results from recent clinical trials in patients with advanced lung cancer or breast cancer have not demonstrated significant activities of bexarotene, suggesting further modification of the drug delivery system. As a consequence, there remains a need to find novel drug vehicles to extend its clinical administration.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related RAR/RXR Products

(CAS: 1351452-80-6)

NRX-204647 is a Retinoic acid receptor gamma-selective inverse agonist.

CAS 925701-88-8 Acitretin sodium

Acitretin sodium
(CAS: 925701-88-8)

Acitretin sodium is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. It can be considered one of the treatments of choic...

(CAS: 1433497-19-8)

LY2955303 is a selective Retinoic acid receptor gamma (RAR-γ) antagonist with Ki of 1.09 nM; (RAR-α Ki > 1700 nM; RAR-β Ki > 2980 nM). LY2955303 showed good pha...

(CAS: 259228-72-3)

HX-603 is a RXR agonist.

CAS 859498-05-8 AGN 205728

AGN 205728
(CAS: 859498-05-8)

AGN 205728 is a potent and selective RARγ antagonist and has no inhibiton on RARα and RARβ.

CAS 107430-66-0 CD1530

(CAS: 107430-66-0)

CD1530 is a potent and selective retinoic acid receptor(RAR) agonist with Ki values of 150, 1500 and 2750 nM for RARγ, RARβ and RARα receptors respectively. It ...

CAS 118292-40-3 Tazarotene

(CAS: 118292-40-3)

Tazarotene could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective l...

(CAS: 205252-59-1)

UAB30 is a low-toxicity retinoid X receptor-selective agonist selective for the binding and activation of RXR’s over RAR' s. UAB30 is highly effective in the pr...

CAS 102121-60-8 AM580

(CAS: 102121-60-8)

AM580 is a stable retinobenzoic derivative originally synthesized as a RARα agonist (EC50 values are 0.3, 8.6 and 13 nM for RARα, RARβ and RARγ respectively).

CAS 911110-93-5 Adapalene sodium salt

Adapalene sodium salt
(CAS: 911110-93-5)

Adapalene sodium salt, a synthetic retinoid, is a Retinoic acid receptor agonist (RAR). It is a third-generation topical retinoid primarily used in the treatmen...

CAS 229961-45-9 AGN 194310

AGN 194310
(CAS: 229961-45-9)

A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to...

CAS 153559-49-0 Bexarotene

(CAS: 153559-49-0)

Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.

AGN 195183
(CAS: 367273-07-2)

RX-195183 is an RARα agonist (Kd=3 nM) with potential antineoplastic activity, modulating the transcription of genes responsible for cell differentiation and pr...

CAS 410528-02-8 Palovarotene

(CAS: 410528-02-8)

Palovarotene is a selective retinoic acid receptor gamma(RAR-γ) agonist for the treatment of emphysema. In small animal studies, palovarotene was claimed to rev...

CAS 958295-17-5 AGN 196996

AGN 196996
(CAS: 958295-17-5)

AGN 196996 is a potent and selective antagonist of RARα. It has been reported to selectively bind to RARs (retinoic acid receptors) for RARα, RARβ and RARγ. It...

CAS 4759-48-2 Isotretinoin

(CAS: 4759-48-2)

Isotretinoin, also known as 13-cis retinoic acid and first marketed as Accutane by Hoffmann-La Roche, is an oral pharmaceutical drug primarily used to treat cys...

CAS 94497-51-5 Tamibarotene

(CAS: 94497-51-5)

Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation and apoptosis of HL-60 cells in vitro. It exhibits antiproliferative effe...

CAS 106685-40-9 Adapalene

(CAS: 106685-40-9)

Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little ...

CAS 71441-28-6 TTNPB

(CAS: 71441-28-6)

TTNPB potently and selectively activates retinoic acid receptors (EC50s = 21, 4, and 2.4 nM for RARα, RARβ, and RARγ, respectively). And it does not act on reti...

CAS 65646-68-6 Fenretinide

(CAS: 65646-68-6)

Fenretinide is an orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenreti...

Chemical Structure

CAS 153559-49-0 Bexarotene

Quick Inquiry

Verification code

Featured Items