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. 2021 Apr 27;13(1):1914885. doi: 10.1080/19420862.2021.1914885

Table 2.

Binding affinity and kinetics parameter of trastuzumab and trastuzumab-MMAF conjugates against HER2

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.