N2'-脱乙酰基-N2'-[3-(甲硫基)-1-氧丙基]-五月氨酸
| 中文名称 | N2'-脱乙酰基-N2'-[3-(甲硫基)-1-氧丙基]-五月氨酸 |
|---|---|
| 中文同义词 | N2'-脱乙酰基-N2'-[3-(甲硫基)-1-氧丙基]-五月氨酸;化合物 T12805 |
| 英文名称 | N2'-Deacetyl-N2'-[3-(methylthio)-1-oxopropyl]-maytansine |
| 英文同义词 | N2'-Deacetyl-N2'-[3-(methylthio)-1-oxopropyl]-maytansine;S-methyl DM1;N2'-Deacetyl-N2'-[3-(methylthio)-1-oxopropyl]-maytansine (>90%);Smethyl DM1,S methyl DM1,S-methyl DM-1;Maytansine, N2'-deacetyl-N2'-[3-(methylthio)-1-oxopropyl]- |
| CAS号 | 912569-84-7 |
| 分子式 | C36H50ClN3O10S |
| 分子量 | 752.32 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 912569-84-7.mol |
| 结构式 | ![N2'-脱乙酰基-N2'-[3-(甲硫基)-1-氧丙基]-五月氨酸 结构式](CAS/20211123/GIF/912569-84-7.gif) |
N2'-脱乙酰基-N2'-[3-(甲硫基)-1-氧丙基]-五月氨酸 性质
| 熔点 | >152°C (dec.) |
|---|---|
| 沸点 | 936.9±65.0 °C(Predicted) |
| 密度 | 1.32±0.1 g/cm3(Predicted) |
| 储存条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| 溶解度 | 可溶于氯仿（少许）、甲醇（少许） |
| 酸度系数(pKa) | 9.82±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 灰白色至浅黄色 |
| 稳定性 | 吸湿性 |
|
Maytansinoids
|
S-methyl DM1 is the primary cellular or liver metabolite of antibody-maytansinoid conjugates prepared with thiol-containing maytansinoids DM1.
The half-maximal concentration for inhibition of microtubule assembly for for S-methyl DM1 is 4 μM. At 100 nM S-methyl-DM1 (84%) suppresses dynamic instability more strongly than Maytansine (45%). Tritiated S-methyl-DM1 bound to 37 high-affinity sites per microtubule (K
d
of 0.1 μM).
The concentration dependence curves for the inhibition of cell proliferation by S-methyl DM1 is sigmoidal in shape in MCF7 cells. Minimal inhibition occurred at 200 pM S-methyl DM1, and inhibition is maximal at 3 nM. S-methyl DM1 (IC
50
of 330 pM) is slightly more potent than Maytansine (IC
50
of 710 pM).
S-methyl DM1 induces maxima of 80% accumulation of cells in G2/M as compared with only 30% in controls in MCF7 cells.