MMAE (Monomethyl auristatin E)

Catalog No.S7721 Batch:S772104

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
* <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.)

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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
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