[CAS NO. 139504-50-0] Mertansine

Name: Mertansine
Brand: Arctom Scientific
SKU: HY-19792

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PRODUCTS SPECIFICATIONS [139504-50-0]

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Catalog

HY-19792

Brand

MCE

CAS

139504-50-0

DESCRIPTION [139504-50-0]

Overview

MDL	-
Molecular Weight	738.29
Molecular Formula	C35H48ClN3O10S
SMILES	C[C@]1([C@@](CC(N(C(C=C2C=C3OC)=C3Cl)C)=O)([H])OC([C@H](C)N(C)C(CCS)=O)=O)[C@H]([C@@H]([C@](OC4=O)([H])C[C@]([C@](/C=C/C=C(C)/C2)([H])OC)(N4)O)C)O1

For research use only. We do not sell to patients.

14 Publications Citing Use of MCE

Summary

Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC) ^[1] ^[2] .

IC50 & Target

Maytansinoids

In Vitro

Mertansine is a strong antiproliferative chemotherapeutics toward over 60 types of cancer cell lines ^[3] .
Mertansine (0-1 μg/mL) shows antitumor activity in malignant B16F10 melanoma cells, and inhibits tumor cell growth by inhibiting mitosis when combined with DTX ^[3] .

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

Cell Proliferation Assay

Cell Line:	Malignant B16F10 melanoma cells ^[3]
Concentration:	0, 0.01, 0.1, and 1 μg/mL
Incubation Time:	4 h
Result:	Showed antitumor activity in malignant B16F10 melanoma cells, with an IC ₅₀ of 0.092 μg/mL. Co-delivery of DTX and DM1, both of which inhibit tumor cell growth by inhibiting mitosis, is an effective strategy to achieve a combinatorial anticancer effect.

In Vivo

Mertansine (DM1) has a low maximum-tolerated dose (MTD) of 1 mg/kg ^[3]

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02452554	Children´s Oncology Group\|National Cancer Institute (NCI)	Pleuropulmonary Blastoma\|Recurrent Malignant Peripheral Nerve Sheath Tumor\|Recurrent Neuroblastoma\|Recurrent Rhabdomyosarcoma\|Recurrent Synovial Sarcoma\|Wilms Tumor	October 12, 2015	Phase 2
NCT02254018	Boehringer Ingelheim	Head and Neck Neoplasms	September 2002	Phase 1
NCT02254005	Boehringer Ingelheim	Breast Neoplasms	October 2002	Phase 1
NCT02254031	Boehringer Ingelheim	Breast Neoplasms	July 2003	Phase 1
NCT02254044	Boehringer Ingelheim	Carcinoma, Squamous Cell	October 2003	Phase 1
NCT02420873	M.D. Anderson Cancer Center\|ImmunoGen, Inc.	Leukemia	May 12, 2015	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years

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

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL ( 84.66 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3545 mL	6.7724 mL	13.5448 mL
5 mM	0.2709 mL	1.3545 mL	2.7090 mL
10 mM	0.1354 mL	0.6772 mL	1.3545 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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

Solubility: 2.17 mg/mL (2.94 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (2.82 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (2.82 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Maytansine, N^2′-deacetyl-N^2′-(3-mercapto-1-oxopropyl)-

N^2′-Deacetyl-N^2′-(3-mercapto-1-oxopropyl)maytansine

Maytansinoid DM 1

DM 1

Mertansine

Emtansine

DM1 maytansine