Cat. No.: HY-15162G

Monomethyl auristatin E (GMP)

Name: Monomethyl auristatin E (GMP)
Brand: MedChemExpress
SKU: HY-15162G
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(Synonyms: MMAE (GMP); SGD-1010 (GMP); Vedotin (GMP))

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Monomethyl auristatin E (MMAE) (GMP) is Monomethyl auristatin E (HY-15162) produced by using GMP guidelines. Monomethyl auristatin E is a tubulin polymerization inhibitor.

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CAS No.: 474645-27-7
Formule: C₃₉H₆₇N₅O₇
Masse moléculaire:717.98

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Please store the product under the recommended conditions in the Certificate of Analysis.

Monomethyl auristatin E (GMP) Chemical Structure

CAS No.: 474645-27-7

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Monomethyl auristatin E (MMAE) (GMP) is Monomethyl auristatin E (HY-15162) produced by using GMP guidelines. Monomethyl auristatin E is a tubulin polymerization inhibitor^[1].

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.59 nM Compound: MMAE	Antiproliferative activity against human A549 cells after 4 days by XTT assay Antiproliferative activity against human A549 cells after 4 days by XTT assay	[PMID: 23845743]
A549	EC₅₀	0.0005 μM Compound: Monomethyl auristatin E	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay Antiproliferative activity against human A549 cells after 72 hrs by MTS assay	[PMID: 28972755]
A549	EC₅₀	0.5 nM Compound: Monomethyl auristatin E	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay Antiproliferative activity against human A549 cells after 72 hrs by MTS assay	[PMID: 28972755]
A549	IC₅₀	1.3 nM Compound: 2; MMAE	Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay	[PMID: 29454703]
BT-474	GI₅₀	0.22 nM Compound: 4, MMAE	Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay	[PMID: 25431858]
BXPC-3	GI₅₀	>1.39 nM Compound: 2b	Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
BXPC-3	GI₅₀	>1.39 nM Compound: Desmethylauristatin E	Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay	[PMID: 28895394]
BXPC-3	GI₅₀	>1.39 nM Compound: Desmethylauristatin E	Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay	[PMID: 28926240]
CWR22R	CC₅₀	1.44 nM Compound: MMAE	Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay	[PMID: 34797052]
DU-145	GI₅₀	0.418 nM Compound: 2b	Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
DU-145	GI₅₀	0.418 nM Compound: Desmethylauristatin E	Growth inhibition of human DU145 cells after 48 hrs by SRB assay Growth inhibition of human DU145 cells after 48 hrs by SRB assay	[PMID: 28895394]
DU-145	GI₅₀	0.418 nM Compound: Desmethylauristatin E	Growth inhibition of human DU145 cells after 48 hrs by SRB assay Growth inhibition of human DU145 cells after 48 hrs by SRB assay	[PMID: 28926240]
DU-145	IC₅₀	0.55 nM Compound: MMAE	Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay	[PMID: 36327103]
DU-145	IC₅₀	0.62 nM Compound: MMAE	Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay	[PMID: 36327103]
H3396	IC₅₀	0.1 nM Compound: 3; MMAE	Cytotoxicity against human H3396 cells assessed as inhibition of cell growth incubated for 96 hrs by Alamar blue assay Cytotoxicity against human H3396 cells assessed as inhibition of cell growth incubated for 96 hrs by Alamar blue assay	[PMID: 39068862]
HEK-293T	IC₅₀	0.068 nM Compound: MMAE	Cytotoxicity against HEK293T cells assessed as inhibition in cell growth Cytotoxicity against HEK293T cells assessed as inhibition in cell growth	[PMID: 33974423]
HeLa	IC₅₀	1 nM Compound: MMAE	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay	[PMID: 36327103]
HeLa	IC₅₀	1.1 nM Compound: MMAE	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay	[PMID: 36327103]
HGC-27	IC₅₀	7.18 nM Compound: MMAE	Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35932567]
KB	IC₅₀	0.19 nM Compound: MMAE	Antiproliferative activity against human KB cells after 4 days by XTT assay Antiproliferative activity against human KB cells after 4 days by XTT assay	[PMID: 23845743]
KM-20L2	GI₅₀	0.599 nM Compound: 2b	Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
KM-20L2	GI₅₀	0.599 nM Compound: Desmethylauristatin E	Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay	[PMID: 28895394]
KM-20L2	GI₅₀	0.599 nM Compound: Desmethylauristatin E	Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay	[PMID: 28926240]
L1210	IC₅₀	2.1 nM Compound: 2; MMAE	Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay	[PMID: 29454703]
LNCaP	IC₅₀	0.71 nM Compound: MMAE	Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay	[PMID: 36327103]
LNCaP	IC₅₀	0.79 nM Compound: MMAE	Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay	[PMID: 36327103]
MCF7	GI₅₀	0.404 nM Compound: 2b	Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
MCF7	GI₅₀	0.404 nM Compound: Desmethylauristatin E	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 28895394]
MCF7	GI₅₀	0.404 nM Compound: Desmethylauristatin E	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 28926240]
MDA-MB-231	IC₅₀	0.25 nM Compound: MMAE	Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay	[PMID: 23845743]
MDA-MB-361	GI₅₀	0.49 nM Compound: 4, MMAE	Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay	[PMID: 25431858]
MES-SA	IC₅₀	0.096 nM Compound: MMAE	Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth	[PMID: 33974423]
MES-SA/Dx5	IC₅₀	88.19 nM Compound: MMAE	Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth	[PMID: 33974423]
MKN-45	IC₅₀	10.7 nM Compound: MMAE	Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35932567]
NCI-H460	GI₅₀	0.683 nM Compound: 2b	Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
NCI-H460	GI₅₀	0.683 nM Compound: Desmethylauristatin E	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay	[PMID: 28895394]
NCI-H460	GI₅₀	0.683 nM Compound: Desmethylauristatin E	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay	[PMID: 28926240]
NCI-H524	IC₅₀	3.7 nM Compound: MMAE	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 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	[PMID: 30735385]
NCI-N87	GI₅₀	0.54 nM Compound: 4, MMAE	Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay	[PMID: 25431858]
NUGC-4	IC₅₀	10.97 nM Compound: MMAE	Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay	[PMID: 35932567]
PC-3	CC₅₀	0.97 nM Compound: MMAE	Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay	[PMID: 34797052]
SF-268	GI₅₀	0.432 nM Compound: 2b	Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay	[PMID: 28211277]
SF-268	GI₅₀	0.432 nM Compound: Desmethylauristatin E	Growth inhibition of human SF268 cells after 48 hrs by SRB assay Growth inhibition of human SF268 cells after 48 hrs by SRB assay	[PMID: 28895394]
SF-268	GI₅₀	0.432 nM Compound: Desmethylauristatin E	Growth inhibition of human SF268 cells after 48 hrs by SRB assay Growth inhibition of human SF268 cells after 48 hrs by SRB assay	[PMID: 28926240]
SK-OV-3	IC₅₀	0.66 nM Compound: 2; MMAE	Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay	[PMID: 29454703]
U-87MG ATCC	EC₅₀	0.0002 μM Compound: Monomethyl auristatin E	Antiproliferative activity against human U87 cells after 72 hrs by MTS assay Antiproliferative activity against human U87 cells after 72 hrs by MTS assay	[PMID: 28972755]
U-87MG ATCC	EC₅₀	0.2 nM Compound: Monomethyl auristatin E	Antiproliferative activity against human U87 cells after 72 hrs by MTS assay Antiproliferative activity against human U87 cells after 72 hrs by MTS assay	[PMID: 28972755]

In Vitro

Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells^[1].
Monomethyl auristatin E (MMAE) sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 474645-27-7
Appearance Solid
Masse moléculaire 717.98
Formule C₃₉H₆₇N₅O₇
Color White to off-white
SMILES

CC(C)[C@H](NC)C(N[C@@H](C(C)C)C(N(C)[C@H]([C@@H](CC(N1[C@]([C@H](OC)[C@H](C(N[C@@H]([C@H](C2=CC=CC=C2)O)C)=O)C)(CCC1)[H])=O)OC)[C@H](CC)C)=O)=O
Synonyms

MMAE (GMP); SGD-1010 (GMP); Vedotin (GMP)
Livraison

Shipping with dry ice.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvant et solubilité

In Vitro:

Ethanol : 50 mg/mL (69.64 mM; Need ultrasonic and warming)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3928 mL

6.9640 mL

13.9280 mL

5 mM

0.2786 mL

1.3928 mL

2.7856 mL

10 mM

0.1393 mL

0.6964 mL

1.3928 mL

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (644 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897. [Content Brief]

[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol	1 mM	1.3928 mL	6.9640 mL	13.9280 mL	34.8199 mL
	5 mM	0.2786 mL	1.3928 mL	2.7856 mL	6.9640 mL
	10 mM	0.1393 mL	0.6964 mL	1.3928 mL	3.4820 mL
	15 mM	0.0929 mL	0.4643 mL	0.9285 mL	2.3213 mL
	20 mM	0.0696 mL	0.3482 mL	0.6964 mL	1.7410 mL
	25 mM	0.0557 mL	0.2786 mL	0.5571 mL	1.3928 mL
	30 mM	0.0464 mL	0.2321 mL	0.4643 mL	1.1607 mL
	40 mM	0.0348 mL	0.1741 mL	0.3482 mL	0.8705 mL
	50 mM	0.0279 mL	0.1393 mL	0.2786 mL	0.6964 mL
	60 mM	0.0232 mL	0.1161 mL	0.2321 mL	0.5803 mL

Bioz

Keywords

Monomethyl auristatin E (GMP)

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Monomethyl auristatin E (GMP)