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Cidofovir DNA/RNA Synthesis inhibitor

Cat. No.: S1516

Cidofovir suppresses virus replication by selective inhibition of viral DNA synthesis.
Cidofovir DNA/RNA Synthesis inhibitor Chemical Structure

Estructura química

Peso molecular: 279.19

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Control de calidad (Quality Control)

Lote: Pureza: 99.97%
99.97

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
HEL cells Function assay Compound was tested for anti-viral activity against HSV-1(KOS) in HEL cells, EC50=0.57 μM
MRC-5 cells Function assay Inhibitory activity against cytopathic effect of HSV-2(E 194) in MRC-5 cells, IC50=10 μM
NHDF cells Function assay Inhibitory activity against replication of HCMV in NHDF cells, IC50=0.5 μM
HFF cells Function assay Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as reduction in cytopathogenicity, EC50=3.2 μM
HFF cells Function assay Antiviral activity against Cowpox virus Brighton in HFF cells assessed as reduction in cytopathogenicity, EC50=7.1 μM
HFF cells Function assay Antiviral activity against vaccinia virus Copenhagen measured as cytopathogenicity in HFF cells, EC50=6.9 μM
bone marrow cells Cytotoxicity assay Cytotoxicity against human bone marrow cells assessed as inhibition of colony forming unit of granulocyte/macrophage, IC50=10 μM
HFF cells Function assay Antiviral activity against Human CMV T2241 in HFF cells by SEAP assay, IC50=0.3 μM
MRC5 cells Function assay Antiviral activity against Human CMV Towne in MRC5 cells by PRA, IC50=0.3 μM
UC1B cells Function assay Antiviral activity against Murine polyomavirus MN/RDE Toronto in mouse UC1B cells assessed as reduction of virus-induced cytopathogenicity, EC50=13 μM
african green monkey Vero cells Function assay Antiviral activity against Herpes simplex virus 1 F infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs, EC50=14.4 μM
HEL cells Function assay 3 days Antiviral activity against HCMV AD169 infected in HEL cells assessed as reduction of virus-induced cytopathogenicity after 3 days, EC50=0.41 μM
HEL cells Function assay 3 days Antiviral activity against HCMV Davis infected in HEL cells assessed as reduction of virus-induced cytopathogenicity after 3 days, EC50=0.41 μM
HFF cells Function assay Antiviral activity against Cytomegalovirus CMV T2211 infected in HFF cells by SEAP reporter gene assay, EC50=0.22 μM
HEL cells Function assay Antiviral activity against ganciclovir-resistant HCMV AD169 clone 4 infected in HEL cells assessed as inhibition of virus-induced cytopathicity, EC50=0.74 μM
HEL cells Function assay Antiviral activity against HCMV Davis infected in human HEL cells assessed inhibition of virus-induced cytopathicity after 7 days postinfection, EC50=0.5 μM
HEL cells Function assay Antiviral activity against HCMV AD169 infected in human HEL cells assessed inhibition of virus-induced cytopathicity after 7 days postinfection, EC50=0.3 μM
HEL cells Function assay Antiviral activity against foscarnet-resistant HCMV AD169 clone C infected in HEL cells assessed as inhibition of virus-induced cytopathicity, IC50=0.045 μM
HFF Proliferation assay 3 days Antiproliferative activity against HFF after 3 days by coulter counter assay, EC50=1.9 μM
HeLaS3 cells Function assay 3-5 days Antiviral activity against Vaccinia virus IHD-J ATCC VR-156 infected in HeLaS3 cells after 3 to 5 days by plaque assay, EC50=18.74 μM
HSB2 cells Function assay 7 days Antiviral activity against Human herpesvirus 6 GS infected in human HSB2 cells assessed as decrease in viral DNA accumulation after 7 days, EC50=2.7 μM
A549 cells Function assay Antiviral activity against Human adenovirus type 11p slobitski infected in A549 cells assessed as inhibition of DNA replication by QPCR assay, EC50=16.5 μM
HFF cells Function assay Antiviral activity against Cowpox virus (Brighton Red) infected in human HFF cells assessed as reduction in viral-induced cytopathic effect by neutral red uptake assay, EC50=6.7 μM
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 279.19 Fórmula

C8H14N3O6P

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 113852-37-2 Descargar SDF Almacenamiento de soluciones madre

Sinónimos HPMPC, GS 0504 Smiles C1=CN(C(=O)N=C1N)CC(CO)OCP(=O)(O)O

Solubilidad (Solubility)

In vitro
Lote:

Water : 3 mg/mL

DMSO : Insoluble
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

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)

mg/kg g μL

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)

In vitro

Cidofovir inhibits human cytomegalovirus (HCMV) infection in cultured cells. This compound is inhibitory to CMV plaque formation even when added to the cells at 48 hr post infection with IC50 of 0.9 μg/mL for Davis and 1.6 μg/mL for AD-169 strains,respectively. It also inhibits herpes simplex virus infection. In addition, this chemical blocks cell fusion induced by HSV-1 in monkey kidney cells and blocks the expression of HSV-l-specific proteins and the synthesis of viral DNA.

In vivo

Cidofovir (5 mg/kg/day) subcutaneously for 5 days significantly reduces average virus infectivity titer in blood, spleen, lung and salivary gland in infected guinea pigs. This compound significantly reduces lymphocytosis and average tissue indexe of spleen in infected animals. . It suppresses all manifestations (skin lesions, paralysis of the hind legs, and mortality) of hairless mice infected intracutaneously with HSV-1 or HSV-2. The most remarkable feature of this compound is that a single administration of the compound, even as late as 4 days after infection, conferees significant protection against HSV-1 or HSV-2 infection. This chemical inhibits growth of the highly aggressive melanoma tumor arising from mouse melanoma B16 cells grafted subcutaneously in C57B16/J mice.

Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/2069375/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11069450/

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
NCT04542252 Completed
Drug Drug Interaction
SymBio Pharmaceuticals
 November 9 2020 Phase 1
NCT01610765 Withdrawn
Herpes Simplex Virus
University of Alabama at Birmingham
 January 2016 Phase 1|Phase 2
NCT01816646 Completed
Blood And Marrow Transplantation
M.D. Anderson Cancer Center|Gilead Sciences
 September 2013 Phase 1
NCT00780182 Completed
Healthy
Chimerix|National Institutes of Health (NIH)
 October 2008 Phase 1