Table 7.
Enzyme and cellular IC50 values for select pyrazolo[3,4-d]pyrimidine and imidazo[2,1-b]thiazole-derived insulin-like growth factor 1 receptor/epidermal growth factor receptor/ErbB-2 inhibitors.
| Compound | Enzyme (cellular) IC50 nM | ||
|---|---|---|---|
| IGF-1R | EGFR2* | Erb-B2 | |
| 26° | 52 (41) | 16 (350) | 170 (310) |
| 27a# | 81 (115) | 58 (85) | 54 (94) |
| 27b§ | 12.5 (207) | 31.5 (2300) | 7.5 (340) |
IGF-1R, insulin-like growth factor 1 receptor; EGFR, epidermal growth factor receptor.
*EGFR construct with L858R mutation;
°ELISA assays of receptor auto-phosphorylation, in A431cells for pIGF-1R and pEGFR and N87 cells for pErbB2;
#ELISA assays of receptor auto-phosphorylation, in MiaPaCa cells for pIGF-1R and pEGFR and N87 cells for pErbB2;
§ELISA assays of receptor auto-phosphorylation, in MiaPaCa cells for pIGF-1R and pEGFR and BT474 cells for pErbB2.