| Cas No.: | 203849-91-6 |
| Synonyms: | Demethyldolastatin 10; Monomethylauristatin D; Monomethyl Dolastatin 10 |
| SMILES: | CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@@H](CC2=CC=CC=C2)C3=NC=CS3)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC |
| Formula: | C41H66N6O6S |
| M.Wt: | 771.06 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | MMAD is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugates (ADCs). |
| Target: | Tubulin[1] |
| In Vivo: | The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats[1]. |
| In Vitro: | MMAD (Monomethyl Dolastatin 10) is coupled through a stable oxime-ligation process to yield several near-homogenous antibody-drug conjugates (ADCs) with a drug-to-antibody ratio of ~2.0. The resulting conjugates demonstrate good pharmacokinetic properties, potent in vitro cytotoxic activity against HER2+ cancer cells. When compared with ADCs prepared by cysteine alkylation following native interchain disulfide reduction, site-specific unnatural-amino-acid-based ADCs are shown to have increased in vitro cytotoxicity[1]. |
| References: | [1]. Chudasama V, et al. Recent advances in the construction of antibody-drug conjugates. Nat Chem. 2016 Feb;8(2):114-9. |

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