139504-50-0

Product Details:

CasNo： 139504-50-0

Molecular Formula： C35H48ClN3O10S

Appearance： White to light yellow crystalline solid

Delivery Time： 2 weeks after order

Throughput： 100KG/Month

Purity： 99%

Synonyms: N2'-deacetyl-N2'-(3-Mercapto-1-oxopropyl)-Maytansine; Maytansinoid dM 1; Maytansine, N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)-; DM1 Compound; DM 1; MAYTANSINOID DM 1
Boiling point: 937.1±65.0 °C
Density: 1.33±0.1 g/cm3
Solubility: DMSO: 60.0(Max Conc. mg/mL); 81.26(Max Conc. mM)
Pka: 9.82±0.70

Description:
Maytansine, a natural alkaloid, was first isolated from Maydens ovale in 1972 and exists in the genus Maydens of the family Weedaceae and its relatives. The mechanism of action of maytansine, acting on microtubules and tubulin, blocks the formation of spindles in the process of cell mitosis by inhibiting the depolymerization of cell microtubules, and has a strong ability to inhibit tumor cell proliferation.

Uses: 
Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. It can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).

Definition:
Mertansine is an organic heterotetracyclic compound and 19-membered macrocyclic lactam that is maytansine in which one of the hydrogens of the terminal N-acetyl group is replaced by a sulfanylmethyl group. It has a role as an antineoplastic agent and a tubulin modulator. It is an alpha-amino acid ester, a carbamate ester, an epoxide, an organic heterotetracyclic compound, an organochlorine compound, a thiol and a maytansinoid. It derives from a maytansine.

Biological Activity:
Mertansine is a thiol-containing derivative of maytansine that is cytotoxic to human epidermoid carcinoma KB and human breast cancer SK-BR-3 cells (IC50 = 1.10 nM for both). Formulations containing mertansine have been studied for the treatment of multiple myeloma and squamous cell carcinoma.