S-methyl DM1

S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin(Kd of 0.93 μM) and inhibts microtubule polymerization.

产品编号 T12805Cas号 912569-84-7

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产品编号 T12805Cas号 912569-84-7

S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin(Kd of 0.93 μM) and inhibts microtubule polymerization.

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产品描述	S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin(Kd of 0.93 μM) and inhibts microtubule polymerization.
靶点活性	Tubulin:(kd)0.93 μM
体外活性	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 (Kd of 0.1 μM)[1]. Minimal inhibition occurred at 200 pM S-methyl DM1, and inhibition is maximal at 3 nM. S-methyl DM1 (IC50 of 330 pM) is slightly more potent than Maytansine (IC50 of 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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