Table 2.
Physicochemical properties of the 9a/9b-C225 conjugation reactions and their corresponding conjugate products. Values for the 9b-C225 conjugates are shown in parentheses.
| Conjugate | MWea | (PTX : C225)cb | (PTX : C225)mc | %yieldpd | %CEe | tR (min)f |
|---|---|---|---|---|---|---|
| 225 | 151,800 | 0 | 0 | NAg | NA | 8.1 |
| 11a (11e) | 158,298 (158,050) | 5 | 2 (2) | 77 (72) | 40 (60) | 8.08 (8.02) |
| 11b (11f) | 162,625 (169,414) | 10 | 3 (5) | 90 (86) | 30 (50) | 8.00 (8.00) |
| 11c (11g) | 171,763 (173,674) | 20 | 5 (6) | 88 (86) | 25 (35) | 7.91 (7.94) |
| 11d (11h) | 198,575 (188,800) | 50 | 12 (10) | 96 (92) | 24 (20) | 7.75 (7.77) |
a
measured by MALDI-TOF MS
b
calculated stoichiometric ratios
c
measured ratios from MALDI-TOF MWs and Equation 1
d
%yield of protein recovery
e
conjugation efficiency, calculated from (PTX : C225)m/(PTX : C225)c • 100
f
SEC-HPLC retention times at 280 nm
g
NA: not applicable