TRK-IN-13 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-13 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-24)[1].
Recifercept (TA-46) is a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule. Recifercept can be used as a decoy/ligand trap to decrease the amount of fibroblast growth factors that can bind to mutant FGFR3 receptors. Recifercept can be used for the research of achondroplasia[1].
PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels[1].
Cetuximab sarotalocan (Cetuximab-IRDye-700DX) is an IRdye700DX (near-infrared photosensitizing dye) conjugate of Cetuximab (anti-EGFR monoclonal antibody). Cetuximab sarotalocan can be used for head and neck cancers research[1][2].
TRK-IN-21 (5n) is an orally activity TRK inhibitor. TRK-IN-21 inhibits TRKAWT, TRKAG667C, TRKAF589L, and TRKAG595 with IC50s of 0.3, 2.3, 0.4 and 0.5 nM, respectively. TRK-IN-21 can be used for the research of cancer[1].
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor[1].
Lavendustin C is a potent Ca2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60c-src(+) kinase (IC50=0.5 µM) [1][2].
PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR with an IC50 of 450 pM[1].
Edralbrutinib is a potent BTK inhibitor[1].
Btk inhibitor 1 is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
Aprutumab (BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has the potential for solid tumors research[1].
EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB[1].
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].
MRX-2843 is an orally available small-molecule inhibitor of both MERTK and FLT3.
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity[1].
FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively[1].
SU11274 is a selective Met inhibitor with IC50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.
2-Hydroxy-3-methylanthraquinone (compound 1) is a natural compound isolated from a water extract of Hedyotis diffusa WILLD. 2-Hydroxy-3-methylanthraquinone shows inhibitory activity against protein tyrosine kinases v-src and pp60src, and induces growth arrest and apoptosis in the HepG2 cancer cells[1].
Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in in vitro assay.
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1].
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.
Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].
PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), and used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas.
Rogaratinib is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor.
4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling[1].
Antiproliferative against-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative against-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative against-5 can be used for researching anticancer[1].
VEGFR-2-IN-37 (compound 12) is an inhibitor of VEGFR-2. The inhibition rate at 200 μM was approximately 56.9 μM. VEGFR-2-IN-37 is a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation[1].
Infigratinib (BGJ-398) is a potent inhibitor of the FGFR family with IC50s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Coprelotamab (GB-221) is an IgG-κ monoclonal antibody targeting EGFR2. The commonly used expression system for Coprelotamab is CHO DG44 (Chinese Hamster Ovary) cells[1].