Name | MMAF-OMe |
---|---|
Synonyms |
L-Valinamide, N-methyl-L-valyl-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-3-[[(1S)-2-methoxy-2-oxo-1-(phenylmethyl)ethyl]amino]-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-
N-Methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-3-{[(2S)-1-methoxy-1-oxo-3-phenyl-2-propanyl]amino}-2-methyl-3-oxopropyl]-1-pyrrolidinyl}-5-methyl-1-oxo-4-heptanyl]-N-methyl-L-valinamide |
Description | MMAF-Ome belongs to ADC, and inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively. |
---|---|
Related Catalog | |
In Vitro | 2.5F-Fc and 2.5F-Fc-MMAF have similar IC50 values (6.9±1.1 vs. 8.3±1.3 nM, respectively), indicating that MMAF conjugation has negligible impact on integrin-binding affinity[1]. |
Cell Assay | Cells are seeded in a 96-well plate at a density of 2,000 cells per well and grown overnight at 37°C, 5% CO2 in the media described for each cell line above. Cells are subsequently treated with 100 μL of fresh media, containing varying concentrations of knottin-Fc fusion proteins or linker-modified MMAF, and incubated for 5 days at 37°C, 5% CO2. Cell proliferation is measured using the Cell Counting Kit-8 (CCK-8), by adding the water-soluble tetrazolium salt, WST-8, to each well in an amount equal to 10% of the culture volume. After incubation for 1 hour at 37°C, absorbance at 450 nm is measured with a Synergy H4 microtiter plate reader. Cell proliferation is expressed as a percentage of absorbance relative to the control of untreated cells. Percent maximum proliferation is then reported as (sample − background)/(control − background) × 100. Error bars represent the SD of experiments performed in triplicate. |
References |
Density | 1.1±0.1 g/cm3 |
---|---|
Boiling Point | 871.8±65.0 °C at 760 mmHg |
Molecular Formula | C40H67N5O8 |
Molecular Weight | 745.989 |
Flash Point | 481.0±34.3 °C |
Exact Mass | 745.498962 |
LogP | 4.66 |
Vapour Pressure | 0.0±0.3 mmHg at 25°C |
Index of Refraction | 1.513 |
Storage condition | 2-8℃ |