Name: MMAE (Monomethyl auristatin E)
Brand: Selleck Chemicals
SKU: S7721
Rating: 5 (8 reviews)

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Control de calidad

Lote: Pureza: 99.99%

99.99

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Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
KB	Antiproliferative assay		4 days	Antiproliferative activity against human KB cells after 4 days by XTT assay, IC50=0.00019μM	23845743
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	23845743
A549	Antiproliferative assay		4 days	Antiproliferative activity against human A549 cells after 4 days by XTT assay, IC50=0.00059μM	23845743
non-small cell lung cancer cells	Cytotoxicity assay	0.5 to 1 nM	4 days	Cytotoxicity against human non-small cell lung cancer cells at 0.5 to 1 nM after 4 days by XTT assay	23845743
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	25431858
MDA-MB-361	Cytotoxicity assay			Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay, GI50=0.00049μM	25431858
NCI-N87	Cytotoxicity assay			Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay, GI50=0.00054μM	25431858
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	28211277
DU145	Growth inhibition assay		48 hrs	Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay, GI50=0.000418μM	28211277
SF268	Growth inhibition assay		48 hrs	Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay, GI50=0.000432μM	28211277
KM20L2	Growth inhibition assay		48 hrs	Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay, GI50=0.000599μM	28211277
NCI-H460	Growth inhibition assay		48 hrs	Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay, GI50=0.000683μM	28211277
HCT116	Function assay	0.5 mM	24 hrs	Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis	28895394
DU145	Growth inhibition assay		48 hrs	Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.000418μM	28895394
SF268	Growth inhibition assay		48 hrs	Growth inhibition of human SF268 cells after 48 hrs by SRB assay, GI50=0.000432μM	28895394
KM20L2	Growth inhibition assay		48 hrs	Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay, GI50=0.000599μM	28895394
NCI-H460	Growth inhibition assay		48 hrs	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay, GI50=0.000683μM	28895394
MCF7	Growth inhibition assay		48 hrs	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay, GI50=0.000404μM	28926240
DU145	Growth inhibition assay		48 hrs	Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.000418μM	28926240
SF268	Growth inhibition assay		48 hrs	Growth inhibition of human SF268 cells after 48 hrs by SRB assay, GI50=0.000432μM	28926240
KM20L2	Growth inhibition assay		48 hrs	Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay, GI50=0.000599μM	28926240
NCI-H460	Growth inhibition assay		48 hrs	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay, GI50=0.000683μM	28926240
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	28972755
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, EC50=0.0005μM	28972755
SKOV3	Cytotoxicity assay		2 days	Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.00066μM	29454703
A549	Cytotoxicity assay		2 days	Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.0013μM	29454703
L1210	Cytotoxicity assay		2 days	Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.0021μM	29454703
NCI-H524	Cytotoxicity assay		2 hrs	Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay, IC50=0.0037μM	30735385
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Información química, almacenamiento y estabilidad

Peso molecular	717.98	Fórmula	C₃₉H₆₇N₅O₇	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	474645-27-7	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	SGD-1010			Smiles	CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(C)C(C2=CC=CC=C2)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)NC

Solubilidad

In vitro
Lote:

DMSO : 100 mg/mL (139.27 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 100 mg/mL

Water : 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	5.000mg/ml (6.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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	Cuando se acopla a cAC10, MMAE muestra citotoxicidad selectiva en células CD30⁺ e induce la detención del crecimiento en fase G2/M y la muerte celular a través de la inducción de apoptosis. Cuando se acopla al anticuerpo anti-CD79b, el anti–CD79b-vcMMAE tiene una actividad muy potente y amplia en un gran panel de líneas celulares de LNH in vitro. Cuando se acopla al anticuerpo anti-HER2, el hertuzumab-vc-MMAE también puede ser internalizado eficazmente y eliminar potentemente las células tumorales que sobreexpresan HER2.
In vivo	En el modelo de ALCL Karpas 299, el cAC10-vcMMAE (1 mg/kg, i.v.) induce una regresión tumoral completa y duradera, mientras que el MMAE libre (0,36 mg/kg) no produce actividad antitumoral detectable. En modelos de xenoinjerto de ratón de LNH, el anti–CD79b-vcMMAE (7 mg/kg, p.o.) resulta sorprendentemente en una remisión tumoral completa sostenida.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/12714494/ [2] https://pubmed.ncbi.nlm.nih.gov/19633198/ [3] https://pubmed.ncbi.nlm.nih.gov/26253944/ [4] https://pubmed.ncbi.nlm.nih.gov/28923397/

Información del ensayo clínico

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06395103	Not yet recruiting	B-cell Acute Lymphoblastic Leukemia\|Diffuse Large B-cell Lymphoma\|Burkitt Lymphoma\|Neuroblastoma\|Ewing Sarcoma	Merck Sharp & Dohme LLC	June 4 2024	Phase 1\|Phase 2
NCT06227156	Recruiting	Castration-resistant Prostate Cancer	RemeGen Co. Ltd.	April 8 2024	Phase 1
NCT06265727	Recruiting	Solid Tumor Adult	Corbus Pharmaceuticals Inc.\|CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.	April 1 2024	Phase 1\|Phase 2
NCT06351020	Not yet recruiting	Locally Advanced or Metastatic GC and GCJ Adenocarcinoma	LaNova Medicines Zhejiang Co. Ltd.\|LaNova Medicines Limited	April 1 2024	Phase 3

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MMAE (Monomethyl auristatin E) Agente Antineoplásico

Estructura química

Peso molecular: 717.98