Products Description
English name：Mertansine
CAS number：139504-50-0
Molecular formula: C35H48ClN3O10S
Molecular weight: 738.29
EINECS No
Related categories:
Small molecule inhibitors; pharmaceutical raw substances; small molecule inhibitors, natural products; scientific active drug series; API [for scientific research only]; medical raw materials; drug substance; inhibitors; heterocyccles; medical raw materials; InhChemicalbookibitors; AntibodyDrugConjugates; pharmaceutical API scientific research raw materials; API; pharmaceutical raw materials; organic chemistry; reagents; chemical reagents; scientific research raw materials
The Mol file: 139504-50-0.mol
Structural formula:
The nature of meidenol
Melting point: 190-192℃ (decomposition)
Boiling point: 937.1 ± 65.0 C (Predicted)
Density: 1.33±0.1g/cm3 (Predicted)
Storage conditions: 2-Chemicalbook8 C
Solubility: DMSO: 60.0 (maximum concentration mg/mL); 81.26 (maximum concentration mM)
Aciity coefficient (pK a): 9.82 ± 0.70 (Predicted)
Form: a crystalline solid
Color: White to light yellow
Use and synthesis method of Meddenin
Summary
Metendenin DM1 is a tubulin inhibitor that binds to and suppresses microtubule dynamics. Medonin is an antibody-conjugated medonignin alkaloid used to overcome the systemic toxicity associated with medonin and to enhance tumor-specific delivery.
Physicochemical property
Medenol is solid at room temperature and pressure and can be dissolved in common organic solvents such as ethyl acetate, dichloromethane and alcohol solvents, but has poor solubility in ether solvents and water.
Use
Metenenin DM1 is a novel antibody drug conjugated by trastuzumab and the small molecule microtubule inhibitor DM1 to produce a synergistic anticancer effect. HER 2 overload is observed in 25% – 30% of affected Chemicalbook in patients with primary breast cancer, and trastuzumab is a recombinant DNA-derived humanized monoclonal antibody that is selectively acting on the extracellular site of HER-2. Can be used for the treatment of HER-2-positive advanced metastatic breast cancer.
Meddenin DM1 is a cytotoxin that is used as a cytotoxic component of antibody-drug conjugates.
Preparation method
Agxing at room temperature under argon protection, the dithiothreitol solution was treated with potassium phosphate buffer containing ethylenediaminetetraacetic acid (EDTA), and the reaction was monitored by HPLC within three hours. Acetyl-protected medenin was dissolved in a mixture of ethyl acetate and methanol, and then Chemicalbook potassium phosphate buffer pH 6.0 for EDTA was added to the reaction system. After the reaction, the reaction mixture was extracted with ethyl acetate, combined the organic layer, washed the organic layer with brine, dried with sodium sulfate, filtered to remove the filtrate of desiccant and concentrated the crude residue of meddenol containing thiol. Finally, the crude residue was separated and purified using preparative HPLC.
Bioactivity
Mertansine (DM1) is a tubulin inhibitor and an antibody-conjugated alkaloid used to overcome systemic toxicity with medenin Chemicalbook and enhance tumor-specific delivery. Mertansine Can be linked to monoclonal antibodies to form antibody-conjugated drugs (ADC).
Target spot
Maytansinoids
Hot Tags: mertansine microtubulin inhibitor, China mertansine microtubulin inhibitor suppliers, monomethyl auristatin, Maytasinol Microtubule Assembly Inhibitor, VcMMAE, pharmaceutical product development, mmae auristatin, 108212-75-5
