[CAS NO. 203849-91-6] MMAD
PRODUCTS SPECIFICATIONS [203849-91-6]
DESCRIPTION [203849-91-6]
Overview
| MDL | MFCD25976743 |
|---|---|
| Molecular Weight | 771.06 |
| Molecular Formula | C41H66N6O6S |
| SMILES | O=C([C@H](C)[C@H]([C@]1([H])CCCN1C(C[C@@H](OC)[C@H]([C@@H](C)CC)N(C([C@@H](NC([C@@H](N(C)[H])C(C)C)=O)C(C)C)=O)C)=O)OC)N[C@@H](CC2=CC=CC=C2)C3=NC=CS3 |
Summary
MMAD is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugates ( ADCs ).
IC50 & Target
|
Auristatin |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The resulting antibody-drug conjugates (ADCs) demonstrate complete tumour regression in rodents. They also have an improved toxicology profile in rats [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
DMSO : 24.5 mg/mL ( 31.77 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.2969 mL | 6.4846 mL | 12.9692 mL |
| 5 mM | 0.2594 mL | 1.2969 mL | 2.5938 mL |
| 10 mM | 0.1297 mL | 0.6485 mL | 1.2969 mL |