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Melphalan DNA alkylator químico

Name: Melphalan
Brand: Selleck Chemicals
SKU: S8266
Rating: 5 (25 reviews)

Cat. No.S8266

Melphalan (Alkeran, Sarcolysin, L-PAM) es un derivado de fenilalanina de la mostaza nitrogenada con actividad antineoplásica.Este producto es un producto químico peligroso (toxicidad aguda/inflamable/corrosivo para la piel). Úselo con mascarilla protectora, guantes y ropa.

Melphalan DNA alkylator químico Chemical Structure

Estructura química

Peso molecular: 305.20

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Control de calidad

Lote: Pureza: 99.47%

99.47

Dianas relacionadas	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Otros DNA alkylator Inhibidores	Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466) Tretazicar (CB1954) Treosulfan Semustine

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Tiempo de incubación	Descripción de la actividad
C6 (Rat) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against C6 (Rat) Glioma cell lines, IC50=11 μM
CEM T-lymphocytes	Cytotoxicity assay		Cytotoxicity against CEM T-lymphocytes, IC50=2.47 μM
D283 MR (human) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against D283 MR (human) Glioma cell lines, IC50=16.3 μM
D283 (human) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against D283 (human) Glioma cell lines, IC50=6.8 μM
D341 (human) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against D341 (human) Glioma cell lines, IC50=12.4 μM
K562	Cytotoxicity assay	1 h	In vitro cytotoxic activity against human leukemic cell line K562 after incubation for 1 hour, IC50=30 μM
Jurkat T cells	Cytotoxicity assay		Inhibitory concentration against Human Jurkat T cells, IC50=2.2 μM
L1210 cell	Cytotoxicity assay	72 h	Tested in vitro for the cytotoxicity as number of viable cells against L1210 cell line after 72 hr treatment at conc. of 10E-6, ID50=1.7 μM
LoVo cell	Growth inhibition assay	144 hr	Tested in vitro for inhibition after 144 hr exposure against human colon carcinoma LoVo cell line, IC50=4.09 μM
MCF-7 cells	Cytotoxicity assay		In vitro cytotoxicity activity against MCF-7, IC50=0.3 μM
Molt 4/C8 cells	Cytotoxicity assay		Cytotoxicity against human Molt 4/C8 cells, IC50=3.24 μM
P388 cells	Cytotoxicity assay		Cytotoxicity evaluated against P388 cells, IC50=0.22 μM
MCF-7	Proliferation assay		Antiproliferative activity in MCF-7 human breast cancer cells, IC50=5.7 μM
C6 glioma cell line	Cytotoxicity assay		Cytotoxicity against rat C6 glioma cell line, IC50=12.6 μM
HCT116 cells	Cytotoxicity assay		Cytotoxicity against human HCT116 cells, IC50=30.2 μM
HCT15 cells	Cytotoxicity assay		Cytotoxicity against human HCT15 cells, IC50=36.3 μM
KM12 cells	Cytotoxicity assay		Cytotoxicity against human KM12 cells, IC50=43.7 μM
SW620 cells	Cytotoxicity assay		Cytotoxicity against human SW620 cells, IC50=38.9 Μm
HCC2998 cells	Cytotoxicity assay		Cytotoxicity against human HCC2998 cells, IC50=41.7 μM
SR cells	Cytotoxicity assay		Cytotoxicity against human SR cells, IC50=1.86 μM
HSC2 cells	Cytotoxicity assay		Cytotoxicity against HSC2 cells, CC50=35 μM
HL60 cells	Cytotoxicity assay		Cytotoxicity against human HL60 cells, CC50=6 μM
MOLT3 cells	Function assay	72 h	Antitumor activity against human MOLT3 cells in presence of Penicillin-G-amidase after 72 hrs by XTT assay, IC50=0.3 μM
HepG2 cells	Growth inhibition assay		Growth inhibition of human HepG2 cells, GI50=17 μM
RT4 cells	Cytotoxicity assay	96 h	Cytotoxicity against human RT4 cells after 96 hrs by microtiter assay, IC50=14.25 μM
RT112 cells	Cytotoxicity assay	96 h	Cytotoxicity against human RT112 cells after 96 hrs by microtiter assay, IC50=4.69 μM
5637 cells	Cytotoxicity assay	96 h	Cytotoxicity against human 5637 cells after 96 hrs by microtiter assay, IC50=0.31 μM
KYSE70 cells	Cytotoxicity assay	96 h	Cytotoxicity against human KYSE70 cells after 96 hrs by microtiter assay, IC50=16.16 μM
KYSE510	Cytotoxicity assay	96 h	Cytotoxicity against human KYSE510 cells after 96 hrs by microtiter assay, IC50=8.18 Μm
KYSE520 cells	Cytotoxicity assay	96 h	Cytotoxicity against human KYSE520 cells after 96 hrs by microtiter assay, IC50=10.49 μM
YAPC cells	Cytotoxicity assay	96 h	Cytotoxicity against human YAPC cells after 96 hrs by microtiter assay, IC50=5.95 μM
DAN-G cells	Cytotoxicity assay	96 h	Cytotoxicity against human DAN-G cells after 96 hrs by microtiter assay, IC50=2.65 μM
SISO cells	Cytotoxicity assay	96 h	Cytotoxicity against human SISO cells after 96 hrs by microtiter assay, IC50=1 μM
LCLC-103H cells	Cytotoxicity assay	96 h	Cytotoxicity against human LCLC-103H cells after 96 hrs by microtiter assay, IC50=4 μM
MCF7 cells	Cytotoxicity assay	96 h	Cytotoxicity against human MCF7 cells after 96 hrs by microtiter assay, IC50=3.71 μM
A427 cells	Cytotoxicity assay	96 h	Cytotoxicity against human A427 cells after 96 hrs by microtiter assay, IC50=5.13 μM
Caov3 cells	Cytotoxicity assay	72 h	Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay
NSCLC cells	Cytotoxicity assay	48 hrs	Cytotoxicity against human NSCLC cells assessed as cell growth after 48 hrs by SRB assay, GI50=6.736083 μM
CNSC cells	Cytotoxicity assay	48 hrs	Cytotoxicity against human CNSC cells assessed as cell growth after 48 hrs by SRB assay, GI50=7.58578 μM
mouse FM3A/0 cells	Proliferation assay	48 hrs	Antiproliferative activity against mouse FM3A/0 cells assessed as inhibition of cell growth after 48 hrs by ZF-Coulter Counting, IC50=3.6 μM
CEM/0 cells	Proliferation assay	48 hrs	Antiproliferative activity against human CEM/0 cells assessed as inhibition of cell growth after 48 hrs by ZF-Coulter Counting, IC50=3.5 μM
HeLa cells	Proliferation assay	48 hrs	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 48 hrs by ZF-Coulter Counting, IC5=1.9 μM
INA-6 cells	Cytotoxicity assay		Cytotoxicity against human INA-6 cells assessed as viable fractions using annexin V-FITC/propidium iodide staining by flow cytometry, EC50=2 μM
PBMC cells	Cytotoxicity assay		Cytotoxicity against human PBMC cells assessed as viable fractions using annexin V-FITC/propidium iodide staining by flow cytometry, EC50=3 μM
SH-SY5Y cells	Cytotoxicity assay	72 h	Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay, IC50=5.5 μM
U251 cells	Cytotoxicity assay	5 days	Cytotoxicity against human U251 cells after 5 days by MTT assay, IC50=3 μM
A549 cells	Cytotoxicity assay	5 days	Cytotoxicity against human A549 cells after 5 days by MTT assay, IC50=3 μM
PANC1 cells	Cytotoxicity assay	5 days	Cytotoxicity against human PANC1 cells after 5 days by MTT assay, IC50=3 μM
HT-29 cells	Cytotoxicity assay	5 days	Cytotoxicity against human HT-29 cells after 5 days by MTT assay, IC50=3 μM
DLD1 cells	Cytotoxicity assay	5 days	Cytotoxicity against human DLD1 cells after 5 days by MTT assay, IC50=3 μM
HeLa cells	Cytotoxicity assay	4 days	Cytotoxicity against human HeLa cells after 4 days by Coulter counter analysis, IC50=1.9 μM
FM3A cells	Cytotoxicity assay	2 days	Cytotoxicity against mouse FM3A cells after 2 days by Coulter counter analysis, IC50=3.6 μM
HL-60(TB) cells	Function assay	24 h	Antileukemic activity against human HL-60(TB) cells assessed as inhibition of tumor growth after 24 hrs, IC50=0.38 μM
SR cells	Function assay	24 h	Antileukemic activity against human SR cells assessed as inhibition of tumor growth after 24 hrs, IC50=3.24 μM
L1210 cells	Proliferation assay	2 days	Antiproliferative activity against mouse L1210 cells assessed as inhibition of cell proliferation incubated for 2 days by Coulter counter based assay, IC50=8.6 μM
FM3A cells	Proliferation assay	2 days	Antiproliferative activity against mouse FM3A cells assessed as inhibition of cell proliferation incubated for 2 days by Coulter counter based assay, IC50=3.6 μM
CEM cells	Proliferation assay	3 days	Antiproliferative activity against human CEM cells assessed as inhibition of cell proliferation incubated for 3 days by Coulter counter based assay, IC50=3.5 μM
HeLa cells	Proliferation assay	4 days	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 4 days by Coulter counter based assay, IC50=1.9 μM
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Información química, almacenamiento y estabilidad

Peso molecular	305.20	Fórmula	C₁₃H₁₈Cl₂N₂O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	148-82-3	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Alkeran, Sarcolysin, L-PAM			Smiles	C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl

Solubilidad

In vitro
Lote:

DMSO : 3.5 mg/mL (11.46 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.

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

In vitro	La exposición de una línea celular de mieloma (RPMI 8226) a un pulso de 30 minutos de melphalan (1-fenilalanina-mostaza) resulta en un retraso en la progresión del ciclo celular característico de los agentes de entrecruzamiento de DNA. Se ha demostrado que este compuesto se une al DNA, RNA y proteínas en células in vitro. Induce aberraciones cromosómicas, intercambio de cromátidas hermanas, micronúcleos, mutaciones en el gen HPRT y DNA Damage en células humanas in vitro. También induce la transformación de células C3H 10T1/2 y otras células. En células de roedores cultivadas, induce aberraciones cromosómicas, intercambio de cromátidas hermanas, mutaciones genéticas y DNA Damage. Además, induce aneuploidía y mutaciones letales recesivas ligadas al sexo en Drosophila, y mutaciones en bacterias.
In vivo	Melphalan ha sido probado en ratones mediante aplicación oral, intraperitoneal y dérmica; en ratas mediante inyección intraperitoneal, y en monos mediante administración oral. En ratones, la administración de este compuesto produjo papilomas de preestómago, linfosarcomas y tumores de piel y pulmón. En ratas, causó tumores de glándulas mamarias y sarcomas peritoneales. Los resultados en monos no fueron concluyentes.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/1915798/ [2] https://pubmed.ncbi.nlm.nih.gov/11695563/ [3] https://www.ncbi.nlm.nih.gov/books/NBK304320/

Información del ensayo clínico

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06313502	Not yet recruiting	Plasma Cell Disorder	University of Arkansas\|University of Iowa	June 2024	Phase 1
NCT04455139	Terminated	Eye Cancer Retinoblastoma	Prof. Beck Popovic Maja\|University of Lausanne Hospitals	November 15 2021	Phase 2
NCT04945954	Not yet recruiting	Hematopoietic Stem Cell Transplantation	Seoul National University Hospital\|National Institute of Food and Drug Safety Evaluation (Republic of Korea)	June 2021	Not Applicable

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Instrucciones de manipulación

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