.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 322.42 INH6 es un potente inhibidor de Hec1, que interrumpe específicamente la interacción Hec1 / Nek2 y provoca desalineación cromosómica. \ n Actividad biológica
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Description
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INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
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Targets
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Hec1 [1]
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In vitro
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INH6 effectively targets the Hec1/Nek2 complex for degradation, and shows potent cell killing activity with IC50 of 1.7, 2.1, 2.4, and 2.5 μM in MDA-MB231, MDA-MB468, HeLa and K562 cell lines. INH6 also triggers mitotic abnormalities in HeLa cells, and induces apoptosis.
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In vivo
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Features
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Protocolo (solo como referencia) Ensayo celular: [1]
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Cell lines
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MDA-MB231, MDA-MB468, HeLa and K562 cell lines
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Concentrations
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~40 μM
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Incubation Time
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4 days
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Method
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Standard XTT assays with a four-day drug treatment procedure are performed to measure the dose-dependent cytotoxicity of INH analogs in cultured cells. Triplicate sets are measured and compiled for final data presentation. The assay is performed by using a commercial kit following the instructions. In principle, cells are plated on 96-well dishes one day before the drug treatment, followed by drug treatment on day 2 and XTT assay on day 5 after drug addition. The absorption at 595 nm is measured with a plate reader and converted to cell survival percentages in comparison to mock treated groups.
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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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\ n Información química
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Molecular Weight (MW)
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322.42
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Formula
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C19H18N2OS
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CAS No.
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1001753-24-7
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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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64 mg/mL
heating
(198.49 mM)
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Water
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<1 mg/mL
(
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Ethanol
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11 mg/mL
heating
(34.11 mM)
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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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N-[4-(2,4,6-trimethylphenyl)-2-thiazolyl]-benzamide
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : Señalización citoesquelética > Inhibidor asociado a microtúbulos
