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

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Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Overige ADC Cytotoxin Inhibitoren	Triptolide SN-38 Luteolin (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Harmine hydrochloride Luteoloside

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	717.98	Formule	C₃₉H₆₇N₅O₇	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	474645-27-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (139.27 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

In vitro	Wanneer gekoppeld aan cAC10, vertoont MMAE selectieve cytotoxiciteit in CD30⁺ cellen, en induceert het G2/M-fase groeistilstand en celdood door inductie van apoptose. Wanneer gekoppeld aan anti-CD79b-antilichaam, heeft anti–CD79b-vcMMAE een zeer krachtige en brede activiteit over een groot aantal NHL-cellijnen in vitro. Wanneer gekoppeld aan anti-HER2-antilichaam, kan hertuzumab-vc-MMAE ook effectief worden geïnternaliseerd en HER2-overexpresserende tumorcellen krachtig doden.
In vivo	In het Karpas 299 ALCL-model induceert cAC10-vcMMAE (1 mg/kg, i.v.) complete, duurzame tumorregressie, terwijl vrij MMAE (0,36 mg/kg) geen detecteerbare antitumoractiviteit produceert. In muizenxenograftmodellen van NHL resulteert anti–CD79b-vcMMAE (7 mg/kg, p.o.) opvallend in langdurige complete tumorremissie.
Referenties	[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/

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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MMAE (Monomethyl auristatin E) Antineoplastisch middel

Chemische structuur

Moleculair gewicht: 717.98