Art. -Nr.: HY-15579

MMAF

(Synonyms: Monomethylauristatin F)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.

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Reinheit: 99.97%
CAS. Nr.: 745017-94-1
Formel: C₃₉H₆₅N₅O₈
Molecular Weight:731.96

Speicherung:

4°C, sealed storage, away from moisture

* The compound is unstable in solutions, freshly prepared is recommended.

MMAF Chemical Structure

CAS. Nr.: 745017-94-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Auristatin

Alle ADC Payloads Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-474	GI₅₀	0.24 nM Compound: 6-OMe, MMAF-OMe	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]
BT-474	IC₅₀	8.8 nM Compound: MMAF	Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay	[PMID: 34676042]
H3396	IC₅₀	105 nM Compound: 39; MMAF	Cytotoxicity against human H3396 cells assessed as cell growth inhibition Cytotoxicity against human H3396 cells assessed as cell growth inhibition	[PMID: 35072477]
H3396	IC₅₀	105 nM Compound: 4; MMAF	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]
HCT-116	IC₅₀	2.88 μM Compound: 39; MMAF	Cytotoxicity against human HCT-116 cells assessed as reduction inc cell viability Cytotoxicity against human HCT-116 cells assessed as reduction inc cell viability	[PMID: 35072477]
HL-60	IC₅₀	137 nM Compound: 39; MMAF	Cytotoxicity against P-gp negative human HL-60 cells assessed as reduction inc cell viability Cytotoxicity against P-gp negative human HL-60 cells assessed as reduction inc cell viability	[PMID: 35072477]
HT-29	IC₅₀	10 nM Compound: 39; MMAF	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition Cytotoxicity against human HT-29 cells assessed as cell growth inhibition	[PMID: 35072477]
MDA-MB-361	GI₅₀	0.21 nM Compound: 6-OMe, MMAF-OMe	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]
NCI-N87	GI₅₀	0.44 nM Compound: 6-OMe, MMAF-OMe	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]
SK-BR-3	IC₅₀	5.3 nM Compound: MMAF	Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay	[PMID: 34676042]

In Vitro

MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC₅₀s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay^[4].

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

In Vivo

The maximum tolerated dose (MTD) in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAE (Monomethylauristatin E) (1 mg/kg). cAC10-L1-MMAF₄ has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF₄ ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively^[4].

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

Chemical Information

CAS. Nr. 745017-94-1
Appearance Solid
Molecular Weight 731.96
Formel C₃₉H₆₅N₅O₈
Color White to off-white
SMILES

CC(C)[C@H](NC)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)C)=O)C(C)C)=O
Synonyms

Monomethylauristatin F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (8)

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Journal Impact Factor

J Control Release

EV20-mediated delivery of cytotoxic auristatin MMAF exhibits potent therapeutic efficacy in cutaneous melanoma. [Abstract]

2018 May 10;277:48-56. PMID: 29550398
Mol Ther Nucleic Acids

Targeted Delivery of Auristatin-Modified Toxins to Pancreatic Cancer Using Aptamers. [Abstract]

2018 Mar 2;10:227-236. PMID: 29499935
Mol Cancer Ther

Payload-binding Fab fragments increase the therapeutic index of MMAE antibody-drug conjugates. [Abstract]

2023 Apr 3;22(4):459-470. PMID: 36723609
Target Oncol

Therapeutic Targeting of Golgi Phosphoprotein 2 (GOLPH2) with Armed Antibodies: A Preclinical Study of Anti-GOLPH2 Antibody Drug Conjugates in Lung and Colorectal Cancer Models of Patient Derived Xenografts (PDX). [Abstract]

2019 Oct;14(5):577-590. PMID: 31541350
Oncol Rep

EV20‑sss‑vc/MMAF, an HER‑3 targeting antibody‑drug conjugate displays antitumor activity in liver cancer. [Abstract]

2021 Feb;45(2):776-785. PMID: 33416143
Research Square Preprint

2023 Dec 4.
University of Minnesota

2022 Sep.
Patent

US20210393733A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 140 mg/mL (191.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.3662 mL

6.8310 mL

13.6619 mL

5 mM

0.2732 mL

1.3662 mL

2.7324 mL

10 mM

0.1366 mL

0.6831 mL

1.3662 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3.5 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.5 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay^[2].

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

Animal Administration^[1]

Mice: When subcutaneous Karpas 299 tumor size reaches 300 mm³, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF₄ or cBR96-L1-MMAF₄ intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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)
Handling Instructions (2659 KB)

Verweise

[1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70. [Content Brief]

[2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4. [Content Brief]

[3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics. [Content Brief]

[4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24. [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

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.3662 mL	6.8310 mL	13.6619 mL	34.1549 mL
	5 mM	0.2732 mL	1.3662 mL	2.7324 mL	6.8310 mL
	10 mM	0.1366 mL	0.6831 mL	1.3662 mL	3.4155 mL
	15 mM	0.0911 mL	0.4554 mL	0.9108 mL	2.2770 mL
	20 mM	0.0683 mL	0.3415 mL	0.6831 mL	1.7077 mL
	25 mM	0.0546 mL	0.2732 mL	0.5465 mL	1.3662 mL
	30 mM	0.0455 mL	0.2277 mL	0.4554 mL	1.1385 mL
	40 mM	0.0342 mL	0.1708 mL	0.3415 mL	0.8539 mL
	50 mM	0.0273 mL	0.1366 mL	0.2732 mL	0.6831 mL
	60 mM	0.0228 mL	0.1138 mL	0.2277 mL	0.5692 mL
	80 mM	0.0171 mL	0.0854 mL	0.1708 mL	0.4269 mL
	100 mM	0.0137 mL	0.0683 mL	0.1366 mL	0.3415 mL

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MMAF

Toxins for Antibody-Drug Conjugate Research Library

Peptidomimetic Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MMAF

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MMAF

Toxins for Antibody-Drug Conjugate Research Library

Peptidomimetic Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MMAF

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MMAF Related Classifications

HY-15579 Related Classifications