Art. -Nr.: HY-14171

Bexarotene

(Synonyms: LGD1069)

22 Cited Publications

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Based on 22 publication(s) in Google Scholar

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC₅₀s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC₅₀ >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.

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Reinheit: 99.17%
CAS. Nr.: 153559-49-0
Formel: C₂₄H₂₈O₂
Molecular Weight:348.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bexarotene Chemical Structure

CAS. Nr.: 153559-49-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
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Bioz

Biologische Aktivität

Beschreibung

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC₅₀s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC₅₀ >10000 nM)^[1]^[2]^[3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.

Alle RAR/RXR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	26.5 μM Compound: Bexarotene	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
A-375	IC₅₀	28.4 μM Compound: Bexarotene	Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
BT-549	EC₅₀	>56 μM Compound: Bex	Cytotoxicity against human BT549 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human BT549 cells assessed as reduction in cell viability by MTT assay	[PMID: 29287960]
Caco-2	EC₅₀	52 nM Compound: 1, Bexarotene	Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay	[PMID: 19791803]
COS-1	EC₅₀	20 nM Compound: 1, LGD1069	Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay	[PMID: 24900241]
COS-1	EC₅₀	20 nM Compound: Bexarotene	Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay	[PMID: 25815156]
CV-1	EC₅₀	20 nM Compound: 2	Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-gamma Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-gamma	[PMID: 10052980]
CV-1	EC₅₀	25 nM Compound: 2	Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-beta Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-beta	[PMID: 10052980]
CV-1	EC₅₀	28 nM Compound: 2	Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-alpha Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-alpha	[PMID: 10052980]
CV-1	EC₅₀	282 nM Compound: 2	Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta	[PMID: 10052980]
CV-1	EC₅₀	6 nM Compound: 2	Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha	[PMID: 10052980]
CV-1	EC₅₀	648 nM Compound: 2	Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma	[PMID: 10052980]
CV-1	EC₅₀	0.04 μM Compound: 37, LGD1069	Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay	[PMID: 19216008]
CV-1	EC₅₀	118 nM Compound: bexarotene	Agonist activity at RXRalpha LBD (unknown origin) expressed in CV1 cells Agonist activity at RXRalpha LBD (unknown origin) expressed in CV1 cells	[PMID: 26331194]
CV-1	EC₅₀	>10000 nM Compound: 6b	Effective concentration against retinoid receptor isoform (RAR beta) expressed in CV-1 cells Effective concentration against retinoid receptor isoform (RAR beta) expressed in CV-1 cells	[PMID: 8071941]
CV-1	EC₅₀	>10000 nM Compound: 6b	Effective concentration against retinoid receptor isoform (RAR gamma) expressed in CV-1 cells Effective concentration against retinoid receptor isoform (RAR gamma) expressed in CV-1 cells	[PMID: 8071941]
CV-1	EC₅₀	24 nM Compound: 6b	Effective concentration against retinoid receptor isoform (RXR beta) expressed in CV-1 cells Effective concentration against retinoid receptor isoform (RXR beta) expressed in CV-1 cells	[PMID: 8071941]
CV-1	EC₅₀	25 nM Compound: 6b	Effective concentration against retinoid receptor isoform (RXR gamma) expressed in CV-1 cells Effective concentration against retinoid receptor isoform (RXR gamma) expressed in CV-1 cells	[PMID: 8071941]
CV-1	EC₅₀	33 nM Compound: 6b	Effective concentration against retinoid receptor isoform (RXR alpha) expressed in CV-1 cells Effective concentration against retinoid receptor isoform (RXR alpha) expressed in CV-1 cells	[PMID: 8071941]
CV-1	EC₅₀	>10000 nM Compound: 6b	Effective concentration against retinoid receptor isoform (RAR alpha) expressed in CV-1 cells Effective concentration against retinoid receptor isoform (RAR alpha) expressed in CV-1 cells	[PMID: 8071941]
CV-1	EC₅₀	20 nM Compound: Targretin	Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR gamma Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR gamma	10.1016/S0960-894X(97)00437-X
CV-1	EC₅₀	25 nM Compound: Targretin	Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR beta Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR beta	10.1016/S0960-894X(97)00437-X
CV-1	EC₅₀	28 nM Compound: Targretin	Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR alpha Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR alpha	10.1016/S0960-894X(97)00437-X
CV-1	EC₅₀	24 nM Compound: 12b	Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta	10.1016/S0960-894X(97)10079-8
CV-1	EC₅₀	25 nM Compound: 12b	Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma	10.1016/S0960-894X(97)10079-8
CV-1	EC₅₀	33 nM Compound: 12b	Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha	10.1016/S0960-894X(97)10079-8
DU-145	IC₅₀	61.6 μM Compound: bexarotene	Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
FaDu	IC₅₀	29.8 μM Compound: Bexarotene	Cytotoxicity against human FaDu cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human FaDu cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
HEK293	EC₅₀	149 nM Compound: bexarotene	Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay	[PMID: 23707260]
HEK293	EC₅₀	40 nM Compound: Targretin, Bexarotene	Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay	[PMID: 24801499]
HEK-293T	EC₅₀	0.196 μM Compound: 18	Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	0.434 μM Compound: 18	Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
Hep 3B2	IC₅₀	191.8 μM Compound: bexarotene	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
HepG2	IC₅₀	20 μM Compound: 2	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by WST-1 assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by WST-1 assay	[PMID: 33793232]
HGC-27	IC₅₀	32.7 μM Compound: bexarotene	Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
HT-29	IC₅₀	>30 μM Compound: Bexarotene	Cytotoxicity against human HT29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human HT29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
KB	IC₅₀	46.3 μM Compound: bexarotene	Cytotoxicity against bexarotene-resistant human KB cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against bexarotene-resistant human KB cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23707260]
KB	IC₅₀	8.8 μM Compound: bexarotene	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
MCF7	IC₅₀	10.6 μM Compound: Bexarotene	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
MDA-MB-231	EC₅₀	>56 μM Compound: Bex	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay	[PMID: 29287960]
NIH3T3	IC₅₀	18.7 μM Compound: Bexarotene	Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
Sf9	IC₅₀	13.5 μM Compound: 40	Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]
Sf9	IC₅₀	5.9 μM Compound: 40	Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]

In Vitro

Bexarotene selectively binds and activates RXR subtypes with K_d=14±2 nM, 21±4 nM, and 29±7 nM for RXRα, RXRβ, and RXRγ subtypes^[1].
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^[1].
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)^[2].
Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation^[2].
Bexarotene (20 and 40 μM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

The human PCa androgen-independent cell lines PC3 and DU145
Concentration:

5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells.
Incubation Time:

24 and 48 hours
Result:

Showed an antiproliferative effect with the IC₅₀s were 40.62±0.45 µM (PC3) and 50.20±4.10 µM (DU145).

Cell Viability Assay^[2]

Cell Line:

PC3 and DU145 cells
Concentration:

20 and 40 µM
Incubation 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.

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^[1].
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 (p53^wt/wtK-ras^wt/wt, p53^val135/wtK-ras^wt/wt, or p53^wt/wtK-ras^ko/wt). Bexarotene reduces the progression of adenoma to adenocarcinoma by ～50% in both p53^wt/wtK-ras^ko/wt and p53^wt/wtK-ras^wt/wt mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

UL53-3 mice (p53^wt/wtK-ras^wt/wt, p53^val135/wtK-ras^wt/wt, or p53^wt/wtK-ras^ko/wt)^[3]
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 153559-49-0
Appearance Solid
Molecular Weight 348.48
Formel C₂₄H₂₈O₂
Color White to off-white
SMILES

CC1(C2=C(C(C)(CC1)C)C=C(C(C(C3=CC=C(C=C3)C(O)=O)=C)=C2)C)C
Synonyms

LGD1069
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (22)

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Journal Impact Factor

Cell

Toward Minimal Residual Disease-Directed Therapy in Melanoma. [Abstract]

2018 Aug 9;174(4):843-855.e19. PMID: 30017245
Nat Commun

RNA nanotherapeutics with fibrosis overexpression and retention for MASH treatment. [Abstract]

2024 Aug 27;15(1):7263. PMID: 39191801
Adv Sci (Weinh)

Retinoic Acid Reprograms Mast Cells Toward a Proinflammatory State to Enhance Antitumor Immunity. [Abstract]

2025 Nov 27:e09340. PMID: 41309490

Bexarotene purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 27:e09340. [Abstract]

Flow cytometry analysis showing HLA-DR and CD40 expression after IFN-γ + TTNPB and IFN-γ + Bexarotene treatment for 48 h.
Int J Biol Macromol

Environmental adaptation in fish induced changes in the regulatory region of fatty acid elongase gene, elovl5, involved in long-chain polyunsaturated fatty acid biosynthesis. [Abstract]

2022 Apr 15:204:144-153. PMID: 35120941
J Med Chem

Design, Synthesis, and Biological Evaluation of Arylimidazole Derivatives as Potent PPARδ Agonists for the Treatment of Renal Fibrosis. [Abstract]

2026 Feb 26;69(4):4469-4492. PMID: 41667192
J Med Chem

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis. [Abstract]

2022 Feb 10;65(3):2571-2592. PMID: 35060744
Neural Regen Res

Bexarotene improves motor function after spinal cord injury in mice. [Abstract]

2023 Dec;18(12):2733-2742. PMID: 37449638

Bexarotene purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Dec;18(12):2733-2742. [Abstract]

Representative HE and Masson staining of spinal cord sections (sagittal) from mice in the sham, SCI, and SCI + Bex (1 mg/kg, i.p.) groups on day 28 after SCI. The dotted line indicates the collagen deposition area.

Bexarotene purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Dec;18(12):2733-2742. [Abstract]

Representative images of immunofluorescence staining for MAP2 (indicating soma and dendrites of neurons, green), NeuN (indicating neurons, red), and SYN (indicating synapse of neurons, green) in spinal cord transverse sections treated with Bex (1 mg/kg, i.p.).

Bexarotene purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Dec;18(12):2733-2742. [Abstract]

Evaluation of CASP1, GSDMD, IL-18, and IL-1β in the spinal cord by ELISA treated with Bex (1 mg/kg, i.p.).

Bexarotene purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Dec;18(12):2733-2742. [Abstract]

Western blot assay of GSDMD-N, NLRP3, Caspase-1, IL-1β, IL-18, and ASC treated with Bex (1 mg/kg, i.p.).
Eur J Med Chem

Design, synthesis, and biological evaluation of imidazolidinone derivatives as potent PPARα/δ agonists for the treatment of cholestatic liver diseases. [Abstract]

2025 Jan 15:286:117284. PMID: 39827490
Eur J Med Chem

Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis. [Abstract]

2024 Apr 5:269:116344. PMID: 38522113
Neurosci Bull

Pharmacological Activation of RXR-α Promotes Hematoma Absorption via a PPAR-γ-dependent Pathway After Intracerebral Hemorrhage. [Abstract]

2021 Oct;37(10):1412-1426. PMID: 34142331
Neurobiol Dis

Bexarotene protects against neurotoxicity partially through a PPARγ-dependent mechanism in mice following traumatic brain injury. [Abstract]

2018 Sep:117:114-124. PMID: 29886067

Bexarotene purchased from MedChemExpress. Usage Cited in: Neurobiol Dis. 2018 Sep:117:114-124. [Abstract]

Bexarotene increases neuronal maintenance and inhibits cell apoptosis after controlled cortical impact (CCI). Representative Western blotting images of cleaved caspase-3, Bax and Bcl-2 in ipsilateral brain on the 14th day after CCI.
Mol Cancer Ther

Inhibition of Integrin αVβ3 Signaling Improves the Antineoplastic Effect of Bexarotene in Cutaneous T-Cell Lymphoma. [Abstract]

2022 Sep 6;21(9):1485-1496. PMID: 35793463
Cells

Redistribution of the SWI/SNF Complex Dictates Coordinated Transcriptional Control over Epithelial-Mesenchymal Transition of Normal Breast Cells through TGF-β Signaling. [Abstract]

2022 Aug 24;11(17):2633. PMID: 36078038
Int J Mol Sci

Molecular Cloning, Characterization, and Nutritional Regulation of Elovl6 in Large Yellow Croaker ( Larimichthys crocea). [Abstract]

2019 Apr 11;20(7). pii: E1801. PMID: 30979053
Eur J Pharmacol

Adapalene suppressed the proliferation of melanoma cells by S-phase arrest and subsequent apoptosis via induction of DNA damage. [Abstract]

2019 May 15:851:174-185. PMID: 30836068
Exp Neurol

Bexarotene promotes microglia/macrophages - Specific brain - Derived Neurotrophic factor expression and axon sprouting after traumatic brain injury. [Abstract]

2020 Dec;334:113462. PMID: 32916173
J Pain

Bexarotent Attenuated Chronic Constriction Injury-Induced Spinal Neuroinflammation and Neuropathic Pain by Targeting Mitogen-Activated Protein Kinase Phosphatase-1. [Abstract]

2020 Nov-Dec;21(11-12):1149-1159. PMID: 30660765
J Pharm Pharmacol

Exploring the combined therapeutic efficacy of bexarotene and icariin in type 2 diabetic rats. [Abstract]

2024 Jul 18:rgae100. PMID: 39024515
Fundam Clin Pharmacol

The third-generation retinoid adapalene triggered DNA damage to induce S-phase arrest in HaCat cells. [Abstract]

2020 Jun;34(3):380-388. PMID: 31808972
Cell Physiol Biochem

Triggering of Suicidal Erythrocyte Death by Bexarotene. [Abstract]

2016;40(5):1239-1251. PMID: 27978526

Bexarotene purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;40(5):1239-1251. [Abstract]

Arithmetic means±SEM (n=14) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) bexarotene (0.2-0.6 µg/mL). For comparison, the effect of the solvent DMSO is shown (grey bar).
Research Square Preprint

2024 Apr 26.
Research Square Preprint

2024 Jan 30.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 60 mg/mL (172.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8696 mL

14.3480 mL

28.6961 mL

5 mM

0.5739 mL

2.8696 mL

5.7392 mL

10 mM

0.2870 mL

1.4348 mL

2.8696 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Nathalia Rodrigues de Almeida, et al. A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397. [Content Brief]

[2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886. [Content Brief]

[3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8696 mL	14.3480 mL	28.6961 mL	71.7401 mL
	5 mM	0.5739 mL	2.8696 mL	5.7392 mL	14.3480 mL
	10 mM	0.2870 mL	1.4348 mL	2.8696 mL	7.1740 mL
	15 mM	0.1913 mL	0.9565 mL	1.9131 mL	4.7827 mL
	20 mM	0.1435 mL	0.7174 mL	1.4348 mL	3.5870 mL
	25 mM	0.1148 mL	0.5739 mL	1.1478 mL	2.8696 mL
	30 mM	0.0957 mL	0.4783 mL	0.9565 mL	2.3913 mL
	40 mM	0.0717 mL	0.3587 mL	0.7174 mL	1.7935 mL
	50 mM	0.0574 mL	0.2870 mL	0.5739 mL	1.4348 mL
	60 mM	0.0478 mL	0.2391 mL	0.4783 mL	1.1957 mL
	80 mM	0.0359 mL	0.1794 mL	0.3587 mL	0.8968 mL
	100 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7174 mL

Keywords

Bexarotene

22 Cited Publications

100 mg Angebot einholen

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Bexarotene

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Publications Citing Use of MedChemExpress (MCE) Bexarotene

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

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Publications (22)

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Complete Stock Solution Preparation Table

Bexarotene Related Classifications

Art. -Nr.: HY-14171