,
|
Volume of the media compartment for MMAE and T-vc-MMAE model, respectively |
ml |
3, 10 |
Fixed |
|
Scaling factor to convert the number of molecules to nanomoles. |
Unitless |
|
Fixed |
,
|
Volume of each cell |
pl |
3.12, 8.14 |
Fixed |
,
|
Doubling time associated with each cell line |
H |
40.1, 33.6 |
Singh et al. (2016b) |
|
Total concentration of intracellular tubulin |
nM |
65 |
Shah et al. (2012) |
,
|
Second-order association and first-order dissociation rates of MMAE binding to tubulin |
1/nM/h, 1/h |
0.0183, 0.545 |
Shah et al. (2012) |
,
|
Second-order association and first-order dissociation rates of T-vc-MMAE binding to HER2 |
1/nM/h, 1/h |
0.37, 0.014 |
Maass et al. (2016) |
|
First-order net antibody-HER2-complex internalization rate |
1/h |
0.11 |
Maass et al. (2016) |
|
First-order nonspecific deconjugation rate of MMAE from ADC |
1/h |
∼0 |
Estimated to be very low value |
|
Average drug/antibody ratio for the formulation of T-vc-MMAE |
Unitless |
4.5 |
Measured in-house |
|
Number of HER2 receptors on N87 and GFP-MCF7 cells, respectively |
Unitless |
950,000, 52,000 |
Measured in-house |
,
|
First-order rate of protease-induced intracellular ADC degradation and MMAE release |
1/h |
0.353 (9%), 0.03 |
Estimated, Maass et al. (2016)
|
|
Average first-order influx rate constant for MMAE from extracellular space to intracellular space for N87 and MCF7 cells. |
1/h |
8.33 (8.5%) |
Estimated |
|
Average first-order efflux rate constants for MMAE from intracellular space to extracellular space for N87 and MCF7 cells. |
1/h |
0.199 (14%) |
Estimated |