Table 2.
Cytotoxic potencies of free cryptophycin‐55 glycinate and cryptophycin‐conjugates against M21 and M21‐L cell lines upon 2 h treatment and 70 h additional incubation.
|
Structure |
IC50 [nM] M21 (αvβ3+) |
IC50 [nM] M21‐L (αv−, αvβ3−) |
|---|---|---|
|
Cry‐55gly (7) |
0.75±0.11 |
0.14±0.08 |
|
cyclo[DKP‐RGD]‐VA‐Cry‐55gly (10) |
72.7±11.2 |
22.3±2.0 |
|
cyclo[DKP‐isoDGR]‐VA‐Cry‐55gly (11) |
122.6±18.6 |
32.6±3.0 |
|
cyclo[DKP‐RGD]‐Cry‐55gly (13) |
261.3±45.8 |
203.0±27.7 |
|
cyclo[DKP‐isoDGR]‐Cry‐55gly (14) |
287.5±35.9 |
140.8±13.3 |