.cp_wz tabla {borde superior: 1px sólido #ccc; borde izquierdo: 1px sólido #ccc; } .cp_wz table td {borde derecho: 1px sólido #ccc; borde inferior: 1px sólido #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} \ n Peso molecular: \ n 361.20 FH535 es un inhibidor de señalización de Wnt / β-catenina y también un antagonista dual de PPARγ y PPARδ. \ n Actividad biológica FH535 antagoniza la transcripción mediada por β-catenina / Tcf e inhibe el reclutamiento de los coactivadores GRIP1 y β-catenina a PPARδ y PPARγ. FH535 muestra un efecto antiproliferación selectivo sobre algunas células cancerosas que expresan una vía alta o activa de Wnt / β-catenina. FH535 aumenta la citotoxicidad del condensado del humo del cigarrillo y provoca cambios en la señalización de β-catenina y EGR-1. FH535 tiene un valor terapéutico potencial en el tratamiento del cáncer de hígado al dirigirse a las células madre del cáncer de hígado y las líneas celulares de carcinoma hepatocelular. Protocolo (solo como referencia) Ensayo de quinasa: [1]
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High-throughput Library Screen
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Three copies of the optimized or mutated Tcf-binding element from TOPFLASH or FOPFLASH driving a secreted alkaline phosphatase reporter gene are cloned into pCEP4 plasmid, replacing the cytomegalovirus promoter. The plasmids are transfected into HepG2 cells, and hygromycin-resistant clones are pooled. Library screening is done at 20 μmol/L concentration in HepG2 serum-free media. Hits are tested in the HCT116 cell line for inhibition of TOPFLASH luciferase activity but not for inhibition of a reporter activity controlled from β-actin promoter.
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Ensayo celular: [1]
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Cell lines
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HCT116, SW48, RKO, LoVo, COLO205, IEC6, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b, Huh7, Fibroblasts
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Concentrations
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30 μM
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Incubation Time
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48 hours
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Method
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Cell viability is determined by the modified 3H-thymidine incorporation assay. Briefly, cells are plated in 96-well microplates for 24 h and treated in triplicate with various concentrations of the test compound. After 48 h of compound exposure, the cells are incubated for an additional 48 h in compound-free medium. The cells are then incubated in medium containing 3H-thymidine for 24 h, washed and mixed with the scintillant in the 96-well plate. Individual wells are counted with a 96-well scintillation counter and the LC50 is calculated.
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Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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Por ejemplo, para modificar la dosis de resveratrol utilizada para un ratón (22,4 mg / kg) a una dosis basada en el BSA para una rata, multiplique 22,4 mg / kg por el factor Km para un ratón y luego divida por el factor Km para una rata. Este cálculo da como resultado una dosis equivalente para ratas de resveratrol de 11,2 mg / kg.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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Información química
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Molecular Weight (MW)
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361.20
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Formula
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C13H10Cl2N2O4S
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CAS No.
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108409-83-2
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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N/A
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Solubility (25°C) *
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In vitro
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DMSO
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72 mg/mL
heating
(199.33 mM)
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Water
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<1 mg/mL
(
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Ethanol
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<1 mg/mL
(
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* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Chemical Name
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2,5-Dichloro-N-(2-methyl-4-nitrophenyl)-benzenesulfonamide
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : Señalización citoesquelética > Inhibidor de Wnt / beta-catenina
