Table 2. Aldehyde Tag Insertion and Payload Conjugation Minimally Affect Antibody FcRn Binding Characteristics, and Show Improved Dissociation at pH 7.3 Relative to α-HER2-DM1.
measured value | α-HER2 untagged | α-HER2 CH1 tag | α-HER2 CT tag | α-HER2 LC tag | α-HER2 CH1 ADC | α-HER2 CT ADC | α-HER2 LC ADC | α-HER2-DM1 ADC |
---|---|---|---|---|---|---|---|---|
KDa (association [nM] at pH 6.0) | 5.2 ± 1.3 | 5.2 ± 1.9 | 5.8 ± 0.7 | 4.7 ± 1.2 | 4.8 ± 1.0 | 4.4 ± 1.1 | 4.8 ± 1.0 | 5.0 ± 0.2 |
% Bound after 5 s at pH 7.3 | 8.6 ± 0.8 | 9.9 ± 1.0 | 9.9 ± 1.7 | 11.0 ± 1.2 | 9.5 ± 0.9 | 12.0 ± 1.4b | 10.9 ± 0.6b | 14.9 ± 0.8c |
Mean KD values are not statistically significantly different as determined by one way ANOVA.
Significantly different from αHER2 untagged, p < 0.03, Two-tailed t-test.
Significantly different from all of the other analytes, p < 0.04, Two-tailed t-test.