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Tyrosine Kinases

A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to a protein in a cell. It functions as an "on" or "off" switch in many cellular functions. Tyrosine kinases are a subclass of protein kinase.The phosphate group is attached to the amino acid tyrosine on the protein. Tyrosine kinases are a subgroup of the larger class of protein kinases that attach phosphate groups to other amino acids (serine and threonine). Phosphorylation of proteins by kinases is an important mechanism in communicating signals within a cell (signal transduction) and regulating cellular activity, such as cell division.

  • Hypericin
    T6S0923548-04-9
    1. Hypericin (Cyclosan) has antineoplastic activity. 2. Hypericin has antibiotic and antiviral activities. 3. Hypericin has antidepressive activity through inhibiting monoamine oxidase enzyme. 4. Hypericin inhibits RANKL-mediated osteoclastogenesis via affecting ERK signalling in vitro and suppresses wear particle-induced osteolysis in vivo.
    • $52
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  • Ruxolitinib
    T1829941678-49-5
    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.
    • $53
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  • Ibrutinib
    T1835936563-96-1
    Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
    • $36
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  • Gefitinib
    T1181184475-35-2
    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.
    • $50
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  • NVP-BSK805 2HCl (1092499-93-8(free base))
    T6294 In house
    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.
    • $53
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  • Larotinib
    T733341438072-11-7
    Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.
    • $74
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  • Tafetinib
    T289111032265-57-8In house
    Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity.
    • $250
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  • SU 4981
    T60094186610-88-8
    SU 4981 is an inhibitor of VEGFR and a modulator of tyrosine kinase activity.
    • $195
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  • Zongertinib
    T695342728667-27-2In house
    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.
    • $148
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  • Vamotinib
    T637461416241-23-0In house
    Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR/ABL and BCR/ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.
    • $133
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  • NVP-AEW541
    T6080475489-16-8
    NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.
    • $41
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  • Pyridone 6
    T3080457081-03-7
    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.
    • $75
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  • Pacritinib
    T6020937272-79-2
    Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
    • $34
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  • Peficitinib
    T6933944118-01-8
    Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
    • $60
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  • Vidarabine
    T15065536-17-4
    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.
    • $38
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    TargetMol | Citations Cited
  • Baricitinib
    T24851187594-09-7
    Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
    • $43
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  • Alectinib
    T19361256580-46-7
    Alectinib (RG-7853) is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.
    • $39
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  • Filgotinib
    T19291206161-97-8
    Filgotinib (GLPG0634) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
    • $50
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  • PP2
    T6266172889-27-9
    PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
    • $39
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  • Geldanamycin
    T634330562-34-6
    Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR) HSP association.
    • $39
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  • Lorlatinib
    T30611454846-35-5
    Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
    • $35
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  • SAR-20347
    T42101450881-55-6
    SAR-20347 is an inhibitor of TYK2, JAK1 2 3 (IC50: 0.6 23 26 41 nM).
    • $32
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  • GSK 3 Inhibitor IX
    T1917667463-62-9
    GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.
    • $37
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  • EGFR-IN-87
    T798881835666-87-9
    EGFR-IN-87 is a potent EGFR tyrosine kinase inhibitor with anticancer activity that inhibits EGFR_d746-750, EGFR_L858R/T790M, and EGFR_WT in A431 cells, and can be used for cancer research.
    • $195
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  • Ginsenoside Ra1
    TN109683459-41-0
    Ginsenoside Ra1 is a component from ginseng. Ginsenoside Ra1 shows significant inhibitory effects on protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation (H/R).
    • $115
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  • Tyrphostin AG30
    T7101122520-79-0
    Tyrphostin AG30 (AG30) (AG30) is a potent protein tyrosine kinases (PTK) inhibitor.
    • $39
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  • Syk Inhibitor II dihydrochloride
    T4391227449-73-2
    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
    • $132
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  • Ilginatinib maleate
    T12266L1354799-87-3
    Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable inhibitor of JAK2.
    • $96
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  • Tyrosine kinase inhibitor
    T171841021950-26-4
    Tyrosine kinase inhibitor is a tyrosine kinase inhibitor used in combination with fragmenting aromatic nitrogen compounds as antiproliferative agents.
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    • Oclacitinib maleate
      T69141640292-55-2
      Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.
      • $33
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    • Brepocitinib
      TQ00101883299-62-4
      Brepocitinib (PF-06700841) is a potent dual JAK1 TYK2 inhibitor (IC50s: 17 nM 23 nM). Brepocitinib also inhibits JAK2 3 (IC50s: 77 nM 6.49 μM).
      • $30
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    • Delgocitinib
      T150961263774-59-9
      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.
      • $172
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    • NDI-034858
      T629022272904-53-5
      NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd<200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases caused by aberrant expression of IL12 and IL23.
      • $263
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    • Ruxolitinib (S enantiomer)
      T6156941685-37-6
      Ruxolitinib S enantiomer (INCB18424) is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
      • $58
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    • GTP-14564
      T7185734823-86-4
      GTP-14564 is a novel tyrosine kinase inhibitor that also inhibits wt-FLT3 and ITD-FLT3. GTP-14564 inhibits the growth of interleukin-3-independent Ba/F1 expressing ITD-FLT3 at 3 μ m, whereas a 30-fold higher concentration of GTP-14564 is required to inhibit the FLT3 ligand-dependent growth (wt-FLT3) of Ba/F3 expressing wild-type FLT3. F3 expressing wild-type FLT3 (wt-FLT3).
      • $39
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    • Ropsacitinib
      T13237L2127109-84-4
      Ropsacitinib (PF-06826647) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain (IC50: 17 nM).
      • $243
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    • Cerdulatinib
      T24871198300-79-6
      Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.
      • $37
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    • Beta-Hydroxyisovalerylshikonin
      TN14407415-78-3
      Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).
      • $139
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    • Cerdulatinib hydrochloride
      T61041369761-01-2
      Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
      • $37
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    • RO495
      T224161258296-60-4
      RO495 (CS-2667), a potent inhibitor of TYK2, inhibits TYK2 with IC50 of 1.5nM as tested in cell-based pharmacological assays
      • $97
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    • Ilginatinib hydrochloride
      T12266L21239358-85-0
      Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable inhibitor of JAK2.
      • $94
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    • ZAP-180013
      T8697873080-25-2
      ZAP-180013 is an inhibitor of zeta-chain-associated protein kinase 70 (ZAP70,IC50 : 1.8 μM).
      • $64
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    • AMG 900
      T6380945595-80-2
      AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A B C with IC50 of 5 nM 4 nM 1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.
      • $44
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    • BMS-911543
      T67901271022-90-2
      BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1 2.
      • $51
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    • TAK-659 hydrochloride
      T42091952251-28-3
      TAK-659 hydrochloride (TAK-659) is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
      • $33
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    • Paltimatrectinib
      T624472353522-15-1
      Paltimatrectinib (PBI-200) is a potent tyrosine kinase inhibitor with anticancer activity that inhibits myosin-related kinase A (TrkA).Paltimatrectinib is used in the study of bladder, breast and colorectal cancers.
      • $199
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    • NVP-BSK805
      T50491092499-93-8
      NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.
      • $57
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    • Baricitinib phosphate
      T23601187595-84-1
      Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1 JAK2 inhibitor.
      • $40
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    • Decernotinib
      T2636944842-54-0
      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.
      • $44
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    • BMS-066
      T14669914946-88-6
      BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
      • $2,420
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