||Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.
||GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
||Tepotinib (EMD 1214063)
||Tepotinib is an inhibitor of MET tyrosine kinase with potential antineoplastic activity.
||Entrectinib is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M r
||LOXO-101 is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
||URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
||SP600125 is a JNK1/2/3 inhibitor (IC50: 40/40/90 nM); 10-fold higher selectivity than MKK4, 25-fold higher selectivity than MKK3, MKK6, PKCα, and PKB.
||Tyrphostin AG 879
||Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
||ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice.
||7,8-Dihydroxyflavone (7,8-DHF) is a naturally-occurring flavone and exist in Tridax procumbens, Godmania aesculifolia, and primula tree leaves.
||GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
||Diosmetin has been found to act as a weak TrkB receptor agonist.
||Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
||Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.
||PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.