S-methyl DM1 是一种美登素 (Maytansine) 的硫代甲基衍生物。S-methyl DM1 以Kd为 0.93 μM 结合微管蛋白并抑制微管聚合。S-methyl DM1 可以有效抑制微管动态不稳定性,并具有抗癌作用。
生物活性 | S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds totubulinwith aKdof 0.93 μM and inhibtsmicrotubulepolymerization. S-methyl DM1 potently suppressesmicrotubuledynamic instability and has anticancer effects[1][2]. |
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体外研究 (In Vitro) | S-methyl DM1 is the primary cellular or liver metabolite of antibody-maytansinoid conjugates prepared with thiol-containing maytansinoids DM1[1]. 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 (Kdof 0.1 μM)[1]. 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 (IC50of 330 pM) is slightly more potent than Maytansine (IC50of 710 pM)[2]. S-methyl DM1 induces maxima of 80% accumulation of cells in G2/M as compared with only 30% in controls in MCF7 cells[2].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |