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S-methyl DM1

Catalog No. T12805   CAS 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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S-methyl DM1 Chemical Structure
S-methyl DM1, CAS 912569-84-7
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,670.00
50 mg 6-8 weeks $ 2,180.00
100 mg 6-8 weeks $ 2,800.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin(Kd of 0.93 μM) and inhibts microtubule polymerization.
Targets&IC50 Tubulin:(kd)0.93 μM
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 (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].
Molecular Weight 752.31
Formula C36H50ClN3O10S
CAS No. 912569-84-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Lopus M, et al. Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules. Mol Cancer Ther. 2010 Oct;9(10):2689-99. 2. Oroudjev E, et al. Maytansinoid-antibody conjugates induce mitotic arrest by suppressing microtubule dynamic instability. Mol Cancer Ther. 2010 Oct;9(10):2700-13.

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Keywords

S-methyl DM1 912569-84-7 Cytoskeletal Signaling Microtubule Associated Smethyl DM1 S methyl DM1 S-methyl DM-1 inhibitor inhibit

 

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