MMAE (Monomethyl auristatin E)

Catalog No.S7721 Batch:S772105

Technical Data

Formula

C₃₉H₆₇N₅O₇

Molecular Weight

717.98

CAS No.

474645-27-7

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (139.27 mM)

Ethanol

100 mg/mL (139.27 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

5.0mg/ml

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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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

Description

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

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]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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).

Cell Assay:^{^[1]}

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).

References

[4] Wang S, et al. Cancer Lett. 2017 Nov 28;409:125-136.

+ Expand

Selleck's MMAE (Monomethyl auristatin E) has been cited by 8 publications

Protein kinase CK2α is overexpressed in classical hodgkin lymphoma, regulates key signaling pathways, PD-L1 and may represent a new target for therapy [ Front Immunol, 2024, 15:1393485]	PubMed: 38807597
Efficacy of retreatment with polatuzumab vedotin in combination with rituximab in polatuzumab vedotin-resistant DLBCL models [ Leuk Lymphoma, 2023, 1-11.]	PubMed: 37548343
The molecular rationale for the combination of polatuzumab vedotin plus rituximab in diffuse large B-cell lymphoma [ Br J Haematol, 2022, 10.1111/bjh.18341]	PubMed: 35764309
Proteogenomic characterization identifies clinically relevant subgroups of intrahepatic cholangiocarcinoma [ Cancer Cell, 2021, S1535-6108(21)00659-0]	PubMed: 34971568
Novel AXL-targeted agents overcome FLT3 inhibitor resistance in FLT3-ITD+ acute myeloid leukemia cells [ Oncol Lett, 2021, 21(5):397]	PubMed: 33777220
Expression and function of protein kinase CK2 in Hodgkin lymphoma [ PaDUA, 2019, N/A]	PubMed: N/A
The two novel DLL4-targeting antibody-drug conjugates MvM03 and MGD03 show potent anti-tumour activity in breast cancer xenograft models [Wang S Cancer Lett, 2017, 409:125-136]	PubMed: 28923397
[ Oncotarget, 2017, ]	PubMed: 28881644

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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