Characteristics of LLP2A Derivatives in Mice
| Cell binding of 111In-DOTA or 64Cu-CB-TE2A LLP2A derivatives | |||||
|---|---|---|---|---|---|
| Derivative (Fig. 1) | Molecular weight (kDa) | (%)/ng* | KA(M−1)† | Dose μg (nM) | Blood AUC (%ID h) |
| LLP2A-DOTA | 1.8 | 25.2 ± 0.5‡ | 2 × 108 | 2 (1); 20 (10) | 22; 24 |
| LLP2A-CB-TE2A | 1.8 | 34.7 ± 0.7 | – | 2 (1) | — |
| LLP2A-DOTA-PEG2,000 | 4.0 | 29.4 ± 1.2 | – | 20 (5) | 24 |
| LLP2A-DOTA-PEG5,000 | 7.5 | 30.7 ± 0.6 | – | 20 (2.5) | 26 |
| LLP2A-DOTA-PEG10,000 | 12.5 | 17.2 ± 1.0 | 6 × 107 | 20 (1.6) | 30 |
| (LLP2A-DOTA)2-PEG10,000 | 14.7 | 24.0 ± 0.5 | 4 × 108 | 20 (1.3) | 33 |
| (LLP2A-DOTA)4-PEG10,000 | 16.8 | 25.4 ± 1.4 | 2 × 109 | 20 (1.1) | 44 |
↵* ng per 106 cells.
↵† Approximate affinity by Scatchard analysis.
↵‡ For 111In-LLP2A-DOTA, Scatchard analysis demonstrated 1.7 × 105 LLP2A target sites per Raji cell.
Molecular weight is given to nearest estimated 0.1 kDa, and nanomoles are given to nearest calculated 0.1 nM.
KA = association constant; AUC = area under the curve.