Olaratumab (IMC-3G3; LY3012207) is an anti-platelet-derived growth factor receptor alpha (PDGFRα) human monoclonal IgG1 antibody with antitumor activity[1].
Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride) is a biosurfactant extracted from Brevibacterium casei LS14.Methyl 12-methyltridecanoate provides a novel approach for functionalizing the silver nanoparticles higher biocompatibility in vivo environmental[1].
YH-306 is a candidate drug in preventing growth and metastasis of colorectal cancer by modulating FAK signalling pathway.
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].
Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Kis of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
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].
Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[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.
Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT[1].
Imatinib is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
Compound cpd-1 is a small molecule Trks inhibitor with good antitumor activity[1].
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively)[1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model[2].
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].
EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC50 of 0.34 μM. EGFR-IN-67 shows anticancer activity[1].
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome[1].
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer[1].
Ficonalkib is a potent inhibitor of Anaplastic lymphoma kinase (ALK), the tyrosine kinase receptor. Ficonalkib, can be used as an antineoplastic agent[1][2].
GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes[1].
GW2580 is an orally bioavailable inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM.
TAM-IN-2 is a TAM inhibitor extracted from patent US 20170275290 A1, pyrrolotriazine compound 0904[1].
VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor with IC50 value of 0.22 µM. VEGFR-2-IN-24 can be used for tumor research[1].
Imatinib Mesylate is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). Ficlatuzumab blocks the activation of the HGF/c-Met signaling pathway, and inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion[1].
1-Naphthyl PP1(1-NA-PP1) hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).IC50 Value:1.0 uM (v-Src); 0.6 uM (c-Fyn); 18 uM (c-Abl) [1]Target: Src Family kinase1-NA-PP1 was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. 1-NA-PP1 was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Overexpression of PKD1 or PKD3 almost completely reversed the growth arrest and the inhibition of tumor cell invasion caused by 1-NA-PP1, indicating that its anti-proliferative and anti-invasive activities were mediated through the inhibition of PKD. Interestingly, a 12-fold increase in sensitivity to 1-NA-PP1 could be achieved by engineering a gatekeeper mutation in the active site of PKD1, suggesting that 1-NA-PP1 could be paired with the analog-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems [2].
Antitumor agent-57 (Compound 3o) is an NQO1-directed antitumor agent. Antitumor agent-57 inhibits tumor cell growth, triggers ROS generation and induces cell apoptosis[1].
Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer[1].
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.