Table 1 Properties of anti-CXCR4 and non-target control ADCs researched in this study.
From: Optimal design, anti-tumour efficacy and tolerability of anti-CXCR4 antibody drug conjugates
ADC designation | mAb (hIgG1) | F(ab) EC50 Jurkat cells (nM) | F(ab) Max MFI Jurkat cells | Location of conjugation site/tag | Type of linker | Linker-payload | DAR | Fc-mediated effector function |
|---|---|---|---|---|---|---|---|---|
513 | m17 | 4.7 | 11461 | CH1 (tag C), CH2 (N297A mutation, site G) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Reduced |
518 | m17 | 4.7 | 11461 | CH2 (N297Q mutation, sites G, H) | Cleavable | AcLys-VC-PABC-0101 | 4 | Reduced |
510 | m17 | 4.7 | 11461 | LC C-term (tag F) | Non-cleavable | AmPEG6C2-Aur0131 | 2 | Active |
519 | m17 | 4.7 | 11461 | LC C-term (tag F) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
381 | m17 | 4.7 | 11461 | HC C-term (tag D) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
553 | h17-NA | 17.1 | 7471 | LC C-term (tag F) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
554 | h17-NS | 5.5 | 12747 | LC C-term (tag F) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
555 | h17-NQ | 17.7 | 7212 | LC C-term (tag F) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
556 | h17-NV.TS | 39.7 | 5015 | LC C-term (tag F) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
669 | h17-NQ | 17.7 | 7212 | LC C-term (tag F) | Non-cleavable | AmPEG6C2-Aur0131 | 2 | Active |
670 | h17-NV.TS | 39.7 | 5012 | LC C-term (tag F) | Non-cleavable | AmPEG6C2-Aur0131 | 2 | Active |
671 | h17-NA | 17.1 | 7471 | LC C-term (tag F) | Non-cleavable | AmPEG6C2-Aur0131 | 2 | Active |
672 | h17-NS | 5.5 | 12747 | LC C-term (tag F) | Non-cleavable | AmPEG6C2-Aur0131 | 2 | Active |
711 | h17-NA | 17.1 | 7471 | CH1 (tag C), CH2 (N297A mutation, site G) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Reduced |
712 | h17-NA | 17.1 | 7471 | LC C-term (tag F), CH1 (tag C) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Active |
713 | h17-NV.TS | 39.7 | 5015 | CH1 (tag C), CH2 (N297A mutation, site G) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Reduced |
714 | h17-NV.TS | 39.7 | 5015 | LC C-term (tag F), CH1 (tag C) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Active |
217 | NNC | N/A | N/A | LC C-term (tag F) | Cleavable | AcLys-VC-PABC-0101 | 2 | Active |
675 | NNC | N/A | N/A | LC C-term (tag F) | Non-cleavable | AmPEG6C2-Aur0131 | 2 | Active |
358 | NNC | N/A | N/A | CH2 (N297Q mutation, sites G, H) | Cleavable | AcLys-VC-PABC-0101 | 4 | Reduced |
560 | NNC | N/A | N/A | CH1 (tag C), CH2 (N297A mutation, site G) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Reduced |
715 | NNC | N/A | N/A | LC C-term (tag F), CH1 (tag C) | Non-cleavable | AmPEG6C2-Aur0131 | 4 | Active |
