pyk2

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

AZ7550 trimesylate salt (AZ7550 Mesylate) is the active metabolite of ositinib, AZ7550 trimesylate salt inhibits IGF1R activity and can be used in the study of non-small cell lung cancer.

Pyk2-IN-2 (compound 13j) acts as a Pyk2 inhibitor, exhibiting an IC 50 value of 0.608 μM for FAK kinase [1].

BT-Amide is an orally active Pyk2 kinase (Pyk2kinase) inhibitor with an IC50 of 44.69 nM. It prevents glucocorticoid-induced bone loss and demonstrates bone-protective activity in C57BL 6 mice.

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.

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-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).

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

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.

PF-4618433 is a selective PYK2 inhibitor with osteogenic activity.

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.

FAK-IN-14 is a highly effective focal adhesion kinase (FAK) inhibitor that induces apoptosis and cell cycle arrest. FAK-IN-14 has weak inhibitory effects on Akt, c-kit, MEK1 2 and mTOR, but has significant inhibitory effects on FAK, FGFR1 and Pyk2.

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

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

Conteltinibtetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride form of Conteltinib. It acts as an inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. When used in combination with Cabozantinib, Conteltinib tetrahydrochloride exhibits a synergistic antitumor effect.

Mps1-IN-1 dihydrochloride, a potent ATP-competitive inhibitor of Mps1 kinase, exhibits an IC50 of 367 nM. It effectively inhibits the activity of Mps1 mitotic kinase and disrupts spindle assembly checkpoint (SAC) function, thereby reducing the viability of both cancerous and 'normal' cells.

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