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

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Control de calidad (Quality Control)

Lote: Pureza: 99.89%

99.89

Dianas relacionadas	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Otros Retinoid Receptor Inhibidores	TTNPB (Arotinoid acid) Tamibarotene AM580 Fenretinide UVI 3003 SR 11237 BMS493 AR7 All trans-Retinal MSU-42011

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	348	Fórmula	C₂₄H₂₈O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	153559-49-0	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	LGD1069			Smiles	CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 70 mg/mL (201.14 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (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.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/12006543/ [2] https://pubmed.ncbi.nlm.nih.gov/19067706/ [3] https://pubmed.ncbi.nlm.nih.gov/18362934/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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)	June 15 2018	Phase 1
NCT01569724	Completed	Hypertriglyceridemia\|Cutaneous T Cell Lymphoma	Rennes University Hospital	January 2012	Phase 4
NCT01001143	Completed	Leukemia Myeloid Acute	Washington University School of Medicine	May 2010	Phase 1
NCT00615784	Terminated	Acute Myeloid Leukemia	Abramson Cancer Center at Penn Medicine	May 25 2010	Phase 2
NCT00125372	Completed	Carcinoma Non-small-cell Lung	Dartmouth-Hitchcock Medical Center\|Ligand Pharmaceuticals\|Genentech Inc.	December 2005	Not Applicable
NCT00316030	Completed	AML\|Acute Myeloid Leukemia	Abramson Cancer Center at Penn Medicine	January 2004	Phase 1

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Bexarotene Retinoid Receptor agonist

Estructura química

Peso molecular: 348