Name | SMCC-DM1 |
Synonyms | DM1-SMC DM1 SMCC SMCC-MDC DM1-SMCC SMCC-DM1 DM1SMCC SMCC-DM1 (DM1-SMCC) N2'-Deacetyl-N2'-[3-[[1-[[4-[[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl]cyclohexyl]methyl]-2,5-dioxo-3-pyrrolidinyl]thio]-1-oxopropyl]-maytansine Maytansine, N2'-deacetyl-N2'-[3-[[1-[[4-[[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl]cyclohexyl]methyl]-2,5-dioxo-3-pyrrolidinyl]thio]-1-oxopropyl]- |
CAS | 1228105-51-8 |
Molecular Formula | C51H66ClN5O16S |
Molar Mass | 1072.61 |
Density | 1.41±0.1 g/cm3(Predicted) |
Melting Point | >166°C (dec.) |
Solubility | DMSO :100 mg/mL (93.23 mM) |
Appearance | Solid |
Color | White to Off-White |
pKa | 9.82±0.70(Predicted) |
Storage Condition | -20°C Freezer |
In vitro study | SMCC-DM1 inhibits HCC1954 and MDA-MB-468 cells proliferation with IC 50 s of 17.2 and 49.9 nM, respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.932 ml | 4.662 ml | 9.323 ml |
5 mM | 0.186 ml | 0.932 ml | 1.865 ml |
10 mM | 0.093 ml | 0.466 ml | 0.932 ml |
5 mM | 0.019 ml | 0.093 ml | 0.186 ml |
In Vivo/In vitro studies | The Mouse/human chimeric CD138 specific monoclonal antibody nBT062 and highly cytotoxic maytansine derivatives were studied in vitro and in vivo for multiple myeloma (MM) anti-tumor effect of cells. BT062SPDB-DM4, BT062-SMCC-DM1 and BT062-SPP-DM in vivo activity was examined in mouse MM cell xenograft models in human and severe combined immunodeficiency (SCID) mice, this model is provided with an implanted bone chip-hu model injected with human MM cells (SCID)). The in vivo efficacy of MOLP-8, nBT062-SPDB-DM4 and nBT062-SMCC-DM1 was then evaluated in SCID mice carrying established cd138-positive nBT062-SPP-DM1 human MM cells. Administration of a single intravenous injection of Immunoconjugate at well-tolerated concentrations resulted in significant dose-dependent tumor growth inhibition and tumor regression, as evidenced by stable body weight. nBT062SPDB-DM4 was the most active conjugate tested in this model. In addition, weekly dosing of nBT062-SMCC-DM1 (six doses of 13.8 μg/kg) completely blocked tumor growth during the dosing period. In summary, nBT062-SMCC-DM1, nBT062-SPDB-DM4 and nBT062-SPP-DM1 have in vitro and in vivo antitumor activity on CD138 positive MM cells, which can overcome the protective effect of cytokines and BMSCs Clin Cancer Res. June 15, 2009; 15(12):4028-37. |
biological activity | SMCC-DM1 (DM1-SMCC) is composed of linker SMCC and toxic molecule DM1, it can be used to prepare antibody-conjugated drugs. DM1 (Mertansine), a thiol-containing maytansine alkaloid, is an effective microtubule disrupting agent. |