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Table 2 Small molecule inhibitors of the signaling pathways and their target genes (5)

From: Signaling pathways involved in colorectal cancer progression

Signaling pathways Factors/drugs approved (or) in development Function Target
EGFR–RAS–MAPK Cetuximab EGFR inhibitor EGFR
Panitumumab EGFR inhibitor EGFR
Gefitinib EGFR inhibitor EGFR
Sorafenib Tyrosine kinase inhibitor RAF
Pertuzumab Monoclonal antibody for Her 2 Her2
Erlotinib Receptor tyrosine kinase inhibitor EGFR
Canertinib (CI-1033) Irreversible tyrosine kinase inhibitor EGFR
Lapatinib Tyrosine kinase inhibitor EGFR
Dacomitinib Irreversible EGFR inhibitor EGFR
Sunitinib Receptor tyrosine kinase inhibitor RTKs
PD158780 Tyrosine kinase inhibitor EGFR
Matuzumab (EMD72000) Monoclonal antibody for EGFR EGFR
Vemurafenib (PLX4032) BRAFV600E inhibitor BRAFV600E
Dabrafenib (GSK2118436) BRAFV600E inhibitor BRAFV600E C-RAF
Encorafenib (LGX818) RAF inhibitor BRAFV600E
XL281(BMS-908662) RAF kinases inhibitor RAF
Trametinib (GSK1120212) MEK1/2 inhibitor MEK1/2
Binimetinib MEK1/2 inhibitor MEK1/2
Selumetinib (AZD6244) MEK inhibitor MEK1/2
VX-11e ERK2 inhibitor ERK2
SCH772984 ERK1/2 inhibitor ERK1/2
NOTCH RO4929097 γ Secretase inhibitor γ Secretase
DAPT (GSI-IX) γ Secretase inhibitor γ Secretase
Dibenzazepine (DBZ) γ Secretase inhibitor γ Secretase
LY411575 γ Secretase inhibitor γ Secretase
GSI34 γ Secretase inhibitor γ Secretase
PI3K–Akt–mTOR OSI027 mTOR kinase inhibitor mTOR
MK2206 AKT inhibitor AKT
GSK690693 AKT inhibitor AKT
Everolimus (RAD001) mTOR inhibitor mTOR
Idelalisib (CAL-101) P110 inhibitor P110γ/δ
BGT226 PI3K/mTOR inhibitor mTOR
PI3K inhibitor P110α/β/γ
Dactolisib (NVP-BEZ235) PI3K and mTOR inhibitor mTOR
GSK690693 Akt inhibitor AKT
AZD8055 mTOR inhibitor mTOR
Alpelisib (BYL719) PI3Kα inhibitor PI3Kα
Perifosine Akt inhibitor AKT
SF-1126 Inhibitors of the PI3K pathway PI3K
Pilaralisib (XL147) PI3K inhibitor PI3Kα/β/γ/δ
Triciribine (VQD002) Akt inhibitor AKT
Temsirolimus Kinase Inhibitor mTOR
TGF-β LY2109761 TGF-β receptor inhibitor TGFBRI/II
AP15012 Antisense molecules TGF-β1
AP11014 Antisense molecules TGF-β
Wnt/β-catenin BC2059 β-catenin inhibitor β-catenin
Sulindac Blocking the PDZ domain of the protein Dishevelled Dishevelled
PNU-74654 Wnt/B-catenin inhibitor Wnt/B-catenin