[CAS NO. 745017-94-1] MMAF
PRODUCTS SPECIFICATIONS [745017-94-1]
DESCRIPTION [745017-94-1]
Overview
| MDL | MFCD25976742 |
|---|---|
| Molecular Weight | 731.96 |
| Molecular Formula | C39H65N5O8 |
| SMILES | CC(C)[C@H](NC)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)C)=O)C(C)C)=O |
7 Publications Citing Use of MCE
Summary
MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates ( ADC s) such as vorsetuzumab mafodotin and SGN-CD19A [1] [2] [3] .
IC50 & Target
|
Auristatin |
In Vitro
MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC 50 s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The maximum tolerated dose in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAF (Monomethylauristatin F) (1 mg/kg). cAC10-L1-MMAF 4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF 4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively [4] .
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, sealed storage, away from moisture
* The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
DMSO : 140 mg/mL ( 191.27 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3662 mL | 6.8310 mL | 13.6619 mL |
| 5 mM | 0.2732 mL | 1.3662 mL | 2.7324 mL |
| 10 mM | 0.1366 mL | 0.6831 mL | 1.3662 mL |
References
- [1] Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.
- [2] Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.
- [3] Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.
- [4] Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.
