DM1 (Mertansine, NSC 746543, Maytansinoid DM1) is a potent maytansinoid that binds to the maytansine site on tubulin and inhibits microtubule assembly. It shows IC₅₀ values in the sub‑nanomolar range against HER2‑positive breast cancer cells. DM1 is a sulfhydryl‑containing derivative of maytansine, derived from ansamitocin P‑3 by chemical modification. In research and clinic, it is used as the payload in the ADC trastuzumab emtansine (Kadcyla®) for HER2‑positive breast cancer, and serves as a model for ADC payload development.
DM1
$699.00
CAS Number: 139504-50-0
Synonyms: Mertansine, Emtansine, Maytansinoid DM1, NSC 746543
Mechanism of Action: β-Tubulin Inhibitor (Maytansine site)
| Purity | Size | Price | Stock | Quantity |
|---|---|---|---|---|
| 98% | 200mg | $699.00 | In stock |
Description
Additional information
| Size |
200mg |
|---|---|
| Purity |
98% |
| M.F. |
C₃₅H₄₈ClN₃O₁₀S |
| M.W. |
738.29 |
| Appearance |
White crystalline powder |
| Melting Point |
190-192°C (decomp) |
| Storage |
Short term: 0-4°C (days to weeks); Long term: -20°C (months to years)- |
| Smiles |
CN(C@@HC(=O)O[C@H]1[C@@]2(OC2C@@HC)C)C(CCS)=O- |
| MDL No |
MFCD28398157- |
Biological activity
| Biological target: | Mitosis Regulation; Tubulin (maytansine site); β-Tubulin (Vinblastine/Maytansine site) |
| In vitro activity: | Binds tubulin, inhibits microtubule assembly; IC₅₀ against SK‑BR‑3 ~0.1 nM. Used in T‑DM1 ADC. |
| In vivo activity: | T‑DM1 shows potent antitumor activity in HER2+ breast cancer xenografts and clinical trials. |
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