c-MET

Norleual TFA is a type IV angiotensin (Ang) similar substance and a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. It is also an AT4 antagonist with strong anti-angiogenic activity.

Onartuzumab (MetMAb) is a humanized, affinity-matured monoclonal antibody that inhibits the receptor tyrosine kinase MET. Onartuzumab effectively inhibits HGF binding, receptor phosphorylation and signal transduction. Onartuzumab has antibody-like pharmacokinetics and anti-tumor activity.

Rilotumumab (AMG 102) is a monoclonal antibody that targets the hepatocyte growth factor (HGF), inhibiting HGF/MET-driven signaling. Rilotumumab has anti-tumor activity and is being studied for use in castration-resistant prostate cancer (CRPC) and solid tumors.

Tunlametinib is an anti-tumor compound and a tyrosine kinase inhibitor.

Entacapone acid (Tyrphostin AG1290) is a tyrosine kinase inhibitor.

Caveolin-1 (82-101) amide (human, mouse, rat) (Caveolin-1 scaffolding domain peptide) is a peptide that reverses aging-associated deleterious changes in multiple organs.

PF-07265807 is a potent TAM and c-Met kinase inhibitor with IC50 values of 6.1 nM, 13.2 nM and 21.6 nM for AXL, MER and TYRO3, respectively.

Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met.

Risvodetinib (IkT-148009) is an oral, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM.

Zongertinib (BI 1810631) is a potent and selective HER2 and EGFR tyrosine kinase inhibitor with IC50 values of 13 nM and 579 nM, respectively.

Adrixetinib is an inhibitor of protein tyrosine kinase with antineoplastic activity.

Emzeltrectinib is a potent tyrosine kinase inhibitor with antineoplastic activity.

MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity.

Canlitinib is a tyrosine kinase inhibitor, extracted from patent WO2018072614 (IV-2).

PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells.

MET kinase-IN-4 is an orally active Met kinase inhibitor.

Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with antitumor activity.

c-Met ligand-1 is a c-Met ligand and component of c-Met PROTAC degrader [1] .

Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor.

HGF-IN-1 ((the compound on the left in the second line of page 77) is a HGF inhibitor.

PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC 50 of 5.4 nM against c-Met and an IC 50 of 3.7 nM against PARP1.

Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti- c-MET antibody.

CYY292 is an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, (IC50s = 5.35, 4.6, 28, 28, and 78 nM, respectively).

ZM 323881 HCl is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.