Name: Bexarotene
Brand: Selleck Chemicals
SKU: S2098
Rating: 5 (19 reviews)

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.89%

99.89

Target correlati	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Altro Retinoid Receptor Inibitori	TTNPB (Arotinoid acid) Tamibarotene AM580 Fenretinide UVI 3003 SR 11237 BMS493 AR7 All trans-Retinal AGN 193109

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	348	Formula	C₂₄H₂₈O₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	153559-49-0	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	LGD1069			Smiles	CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 70 mg/mL (201.14 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	1.750mg/ml (5.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 35 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.862mg/ml (2.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 17.24 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	RXR
In vitro	Bexarotene treatment at 1 mM and 10 mM for 96 h increases the number of cells with sub-G1 populations and annexin V binding in a dose-dependent manner compared with vehicle controls (DMSO) in well-established CTCL cell lines (MJ, Hut78, and HH), respectively. This compound suppresses the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in all three lines compared with untreated controls. It decreases the protein levels of survivin, activates caspase-3, and cleaved poly(ADP-Ribose) polymerase, but has no obvious effect on expression of Fas/Fas ligand and bcl-2 proteins in all three CTCL lines. It induces a loss of viability and more pronounced inhibition of clonogenic proliferation in HH and Hut-78 cells, whereas the MJ line exhibits resistance. The chemical upregulates and activates Bax in sensitive lines, although not enough to signal significant apoptosis. It signals both G(1) and G(2)/M arrest by the modulation of critical checkpoint proteins. It activates p53 by phosphorylation at Ser15, which influences the binding of p53 to promoters for cell cycle arrest, induces p73 upregulation, and, in concordance, also modulates some p53/p73 downstream target genes, such as p21, Bax, survivin and cdc2.
In vivo	Bexarotene significantly prevents ER-negative mammary tumorigenesis with less toxicity than naturally occurring retinoids in animal models. This compound inhibits the development of preinvasive mammary lesions such as hyperplasias and carcinoma-in-situ in MMTV-erbB2 mice.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/12006543/ [2] https://pubmed.ncbi.nlm.nih.gov/19067706/ [3] https://pubmed.ncbi.nlm.nih.gov/18362934/

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2026-02-04)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT05296304	RECRUITING	Cutaneous T-cell Lymphoma	Memorial Sloan Kettering Cancer Center	2022-03-16	PHASE1
NCT04664829	COMPLETED	Metastatic Triple-Negative Breast Carcinoma	National Cancer Centre, Singapore	2020-10-01	PHASE1
NCT05106192	WITHDRAWN	Mycosis Fungoides of Skin (Diagnosis); Cutaneous T-cell Lymphoma; Non Hodgkin Lymphoma; Lymphomatoid Papulosis; Lymphoma, Large-Cell, Anaplastic; Lymphoma, Follicular	Case Comprehensive Cancer Center	2022-04-01
NCT03323658	COMPLETED	Breast Atypical Ductal Hyperplasia; Breast Atypical Lobular Hyperplasia; Breast Ductal Carcinoma In Situ; Breast Lobular Carcinoma In Situ; Invasive Breast Carcinoma	National Cancer Institute (NCI)	2018-06-15	PHASE1
NCT03323658	Completed	Breast Atypical Ductal Hyperplasia\|Breast Atypical Lobular Hyperplasia\|Breast Ductal Carcinoma In Situ\|Breast Lobular Carcinoma In Situ\|Invasive Breast Carcinoma	National Cancer Institute (NCI)	2018-06-15	Phase 1
NCT00411632	COMPLETED	Lung Cancer	M.D. Anderson Cancer Center	2006-11-29	PHASE2

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C8=C7/X	C8:	LOG(C8):

Bexarotene Retinoid Receptor Agonista

Peso molecolare: 348