| CAS NO: | 203849-91-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Name: MMAD CAS#: 203849-91-6 Chemical Formula: C41H66N6O6S Exact Mass: 770.4765 Molecular Weight: 771.075 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: Monomethylauristatin D; MMAD, Demethyldolastatin 10; Monomethyl Dolastatin 10; Chemical Name: (S)-N-((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide InChi Key: BLUGYPPOFIHFJS-UUFHNPECSA-N InChi Code: InChI=1S/C41H66N6O6S/c1-12-27(6)36(46(9)41(51)35(26(4)5)45-39(50)34(42-8)25(2)3)32(52-10)24-33(48)47-21-16-19-31(47)37(53-11)28(7)38(49)44-30(40-43-20-22-54-40)23-29-17-14-13-15-18-29/h13-15,17-18,20,22,25-28,30-32,34-37,42H,12,16,19,21,23-24H2,1-11H3,(H,44,49)(H,45,50)/t27-,28+,30-,31-,32+,34-,35-,36-,37+/m0/s1 SMILES Code: O=C(N[C@@H](CC1=CC=CC=C1)C2=NC=CS2)[C@H](C)[C@H]([C@@]3(CCCN3C(C[C@H]([C@H]([C@H](CC)C)N(C([C@H](C(C)C)NC([C@@H](N(C)[H])C(C)C)=O)=O)C)OC)=O)[H])OC |
| Target | Tubulin[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]. |
| In Vivo | The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats[1]. |
| References | [1]. Recent advances in the construction of antibody-drug conjugates. Nat Chem. 2016 Feb;8(2):114-9. |
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