Insulin Receptor

GSK1904529A selectively inhibits IGF-IR and IR with IC(50)s of 27 and 25 nmol/L, respectively.

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM.

NVP-AEW541 is a selective IGF-1R kinase inhibitor that inhibits the autophosphorylation activity of IGF-1R (IC50 = 0.086 uM) and prevents IGF-1-mediated survival and proliferation of MCF-7 cells (IC50 = 0.16 and 1.64 uM, respectively).

OSI-906 is a potential first-in-class selective small molecule, dual kinase inhibitor of both insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR).

BMS-536924 is an effective inhibitor of IGF-IR, causing a reversion of an IGF-IR - mediated transformed phenotype.

BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.

AG-1024 (Tyrphostin) is a specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity. Exhibits lower IC50 values for IGF-1 than for the insulin receptor. Also inhibits insulin-stimulated cellular proliferation.

NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target.

LDK378 dihydrochloride is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

SU4984 is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 μM).