Table 1.
Representative inhibitors targeting rat sarcoma virus (RAS) downstream effectors.
| Name | Potency | Target | Structure |
|---|---|---|---|
| Dabrafenib/ GSK2118436 |
IC50: 0.6 nM (B-RafV600E) IC50: 5 nM (C-Raf) |
Raf |
|
| PLX7904 | IC50: 5 nM (B-RafV600E) | B-RafV600E |
|
| CH5126766/ RO5126766 |
IC50: 8.2 nM (B-RafV600E) IC50: 190 nM (B-Raf) IC50: 56 nM (C-Raf) IC50: 160 nM (MEK) |
Raf and MEK1/2 |
|
| Trametinib/ GSK1120212 |
IC50: 0.92 nM/1.8 nM (MEK1/2) | Mek1/2 |
|
| Selumetinib/ AZD6244 |
IC50: 14 nM (MEK1) Kd: 530 nM (MEK2 |
MEK1/2 |
|
| Ulixertinib/ BVD-523 |
IC50: <0.3 nM (Erk2) | Erk1/2 |
|
| LY3214996 | IC50: 5 nM (Erk1/2) | Erk1/2 |
|
| Copanlisib/ BAY80 |
IC50: 0.5 nM (PI3Kα) IC50: 0.7 nM (PI3Kδ) IC50: 3.7 nM (PI3Kβ) IC50: 6.4 nM (PI3Kγ) |
Pan-PI3K |
|
| MK-2206 | IC50: 8 nM (Akt1) IC50: 12 nM (Akt2) IC50: 65 nM (Akt3) |
Akt |
|
| AZD8055 | IC50: 0.8 nM (mTOR) | mTORC1 and mTORC2 |
|