Name: Fludarabine (NSC 118218) Phosphate
Brand: Selleck Chemicals
SKU: S1229
Rating: 5 (59 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.91%

99.91

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

Líneas celulares	Tipo de ensayo	Tiempo de incubación	Descripción de la actividad
HL60 cells	Proliferation assay	48 h	Antiproliferative activity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.09 μM
MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.13 μM
KG1 cells	Proliferation assay	48 h	Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.15 μM
Raji cells	Proliferation assay	48 h	Antiproliferative activity against human Raji cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.4 μM
K562 cells	Proliferation assay	48 h	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.4 μM
ZR-75-1 cells	Proliferation assay	48 h	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.6 μM
MOLT3 cells	Proliferation assay	48 h	Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.95 μM
M-HeLa cells	Proliferation assay	48 h	Antiproliferative activity against human M-HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2 μM
SK-UT-1B cells	Proliferation assay	48 h	Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	365.21	Fórmula	C₁₀H₁₃FN₅O₇P	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	75607-67-9	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	F-ara-A Phosphate, NSC 118218 Phosphate			Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)COP(=O)(O)O)O)O)F)N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 73 mg/mL (199.88 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 3 mg/mL

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.
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	DNA polymerase α (Cell-free assay) 1.1 μM(Ki ) DNA polymerase δ (Cell-free assay) 1.3 μM(Ki)
In vitro	Fludarabine Phosphate is converted to F-ara-ATP in cells and then incorporated into DNA in a self-limiting manner. This compound competes with dATP for incorporation into the A site of the extending DNA strand, which results in termination of DNA strand elongation. Human DNA polymerase α incorporates more of this chemical into DNA than polymerase δ. It completively inhibits DNA polymerase α and DNA polymerase δ with K_i of 1.1 μM and 1.3 μM, respectively. DNA polymerase δ is also able to excise the incorporated Fludarabine Phosphate from DNA in vitro.
In vivo	Fludarabine Phosphate is toxic for tumor-free mice. The maximum tolerated dose (LD10) of this compound administered as a single dose is 234 mg/kg. The 50% lethal dose is 375 mg/kg. This chemical administered as a single dose induces fewer number of cells surviving therapy in mice bearing P388 leukemia, accompanied by greater percentage of increase in life span (110%) and increased median survival time.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/1697861/ [2] https://pubmed.ncbi.nlm.nih.gov/6210262/ [3] https://pubmed.ncbi.nlm.nih.gov/7083151/

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
NCT05039892	Not yet recruiting	CholangiocarcinomaAdult	3D Medicines (Beijing) Co. Ltd.\|3D Medicines	December 2024	Phase 2
NCT06377293	Not yet recruiting	End-Stage Kidney Disease	Far Eastern Memorial Hospital	November 2024	Not Applicable
NCT06398002	Not yet recruiting	Secondary Hyperparathyroidism\|End-stage Kidney Disease	Iain Bressendorff\|Herlev Hospital	August 1 2024	Phase 2
NCT06383403	Not yet recruiting	Primary Biliary Cholangitis	Ipsen	July 1 2024	Phase 3
NCT06302439	Not yet recruiting	Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 Deficiency\|ATP-Binding Cassette Subfamily C Member 6 Deficiency	Inozyme Pharma\|GACI Global	May 2024	--

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):

Fludarabine (NSC 118218) Phosphate Inhibidor de la síntesis de ADN/STAT1

Peso molecular: 365.21

Control de calidad (Quality Control)

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

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

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Información del ensayo clínico (Clinical Trial Information)

Fludarabine (NSC 118218) Phosphate Inhibidor de la síntesis de ADN/STAT1

Peso molecular: 365.21

Control de calidad (Quality Control)

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

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

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Información del ensayo clínico (Clinical Trial Information)

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