tyrosinekinases

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.

Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.

Vidarabine (Adenine Arabinoside) is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.

Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23 22 nM, in cell-free assays).

SU 4981 is an inhibitor of VEGFR and a modulator of tyrosine kinase activity.

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.

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

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12 23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.

Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally available kinase inhibitor with antitumor activity that inhibits MET, AXL, RON, and MKNK1/2, and inhibits the growth of NTRK fusion-carrying tumors.

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 values of 10 nM for JAK1, 28 nM for JAK2, 810 nM for JAK3, and 116 nM for TYK2.

Alectinib (RG-7853) is an ALK inhibitor (IC50=1.9 nM, Kd=2.4 nM) that is selective, orally active, and ATP-competitive. Alectinib has antitumor activity and is used in the treatment of non-small cell lung cancer.

Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1 JAK2 inhibitor.

Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.

Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

HNMPA-(AM)3 inhibits activation of ERK phosphorylation and stimulation of ecdysteroid production by prothyrotropin (PTTH). Furthermore, HNMPA-(AM)3 had inhibitory effects on ecdysteroid production (IC50=14.2 μM) and insulin receptor activity (IC50=14.2 μM and 200 μM, in mosquitoes and mammals, respectively).

SAR-20347 is an inhibitor of TYK2 and JAK1/2/3, with IC50 values of 0.6 nM, 23 nM, 26 nM, and 41 nM, respectively.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.