pyk2

AZ7550 hydrochloride (AZ7550 hydrochloride ), an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

PF-562271 besylate (PF-00562271 Besylate) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in K

PF-719 is a potent, selective Pyk2 inhibitor with IC50 of 17 nM.

PF-4618433 is a dual inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2).