Table 2.
Sample | 1st measurement |
2nd measurement |
Avg. KD (nM) | ||||
---|---|---|---|---|---|---|---|
ka (M-1s-1) | kd (s−1) | KD (nM) | ka (M-1s-1) | kd (s−1) | KD (nM) | ||
Trastuzumab | 3.46 E + 05 | 4.32 E-05 | 0.13 | 1.71 E + 05 | 3.75 E-05 | 0.22 | 0.18 |
T-N-F(DAR 1.6) | 2.96 E + 05 | 3.51 E-05 | 0.12 | 9.55 E + 04 | 8.17 E-06 | 0.09 | 0.11 |
T-N-F(DAR 3.2) | 3.81 E + 05 | 3.99 E-05 | 0.11 | 9.44 E + 04 | 6.23 E-06 | 0.07 | 0.09 |
T-C-F (DAR 3.7) | 4.10 E + 05 | 3.74 E-05 | 0.09 | 1.14 E + 05 | 1.62 E-05 | 0.14 | 0.12 |
T-K-F (DAR 3.9) | 5.31 E + 05 | 6.32 E-05 | 0.12 | 9.39E+04 | 2.03E-05 | 0.22 | 0.17 |
MMAF: monomethyl auristatin F, HER2: human epidermal growth factor receptor 2, DAR: drug-to-antibody ratio, T-N-F: trastuzumab-MMAF conjugate synthesized via NTERM conjugation, T-C-F: trastuzumab-MMAF conjugate synthesized via thiol conjugation, T-K-F: trastuzumab-MMAF conjugate synthesized via lysine conjugation.