Home Cytoskeletal Signaling ADC Cytotoxin inhibitor - Microtubule Associated inhibitor MMAE (Monomethyl auristatin E) For research use only.

MMAE (Monomethyl auristatin E)

Synonyms: SGD-1010

MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent .

MMAE (Monomethyl auristatin E) Chemical Structure

MMAE (Monomethyl auristatin E) Chemical Structure

CAS No. 474645-27-7

Purity & Quality Control

MMAE (Monomethyl auristatin E) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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
Click to View More Cell Line Experimental Data

Biological Activity

Description MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent .
In vitro
In vitro

When coupled to cAC10, MMAE shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. [1]

When coupled to anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro. [2]

When coupled to anti-HER2 antibody, hertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells. [3]
Cell Research Cell lines CD30+ Karpas 299 cells
Concentrations ~1000 ng/mL
Incubation Time 96 h
Method

Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT).
In Vivo
In vivo

In the Karpas 299 ALCL model, cAC10-vcMMAE (1 mg/kg, i.v.) induces complete, durable tumor regression, while free MMAE (0.36 mg/kg) doesn’t produce detectable antitumor activity. [1]

In mouse xenograft models of NHL, anti–CD79b-vcMMAE (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

Chemical Information & Solubility

Molecular Weight 717.98 Formula
C39H67N5O7
 
CAS No. 474645-27-7 SDF Download MMAE (Monomethyl auristatin E) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (139.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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