(3S,4R)-PF-6683324 is a tropomyosin-related kinase (Trk) inhibitor extracted from patent WO2015092610A1 example 9. (3S,4R)-PF-6683324 has the potential for the research of pain and cancer[1].
Cinnamtannin B-1 is a proanthocyanidin with multiple biological functions, including antioxidant effects. Cinnamtannin B-1 inhibits RANKL-induced osteoclastogenesis and prevents ovariectomy-induced osteoporosis in vivo[1]. Cinnamtannin B-1 can be used for the research osteoporosis and colon cancers[1][2].
LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455)[2].
RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks Gas6-inducible Axl receptor activation with a low micromolar IC50in cell assays, and suppresses lung cancer tumor growth[1].
Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis[1].
RR-SRC is a substrate for src-tyrosine-specific protein kinase[1].
FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27))[1].
IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with the IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies[1][2].
ERK Inhibitor II (Negative control) is an effective inhibitor of extracellular signal-regulated kinase (ERK). ERK Inhibitor II (Negative control) inhibits the activation of insulin receptor, which can be used in the study of diabetes[1][2].
Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has the potential for cancer research[1].
Tyrosine kinase-IN-4 (EXAMPLE 107) is a protein tyrosine kinase inhibitor[1].
Tarcocimab (OG1953) is a humanized anti-VEGFA monoclonal antibody (IgG1 type). Tarcocimab is available for research in retinal vein occlusion (RVO) and wet age-related macular degeneration (AMD).
CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM.
c-FMS inhibitor is a novel c-Fms kinase inhibitor with a potential as anti-inflammatory agent and antirheumatic agent.IC50 value:Target: c-Fms
PND-1186 is a potent and reversible inhibitor of FAK with an IC50 of 1.5 nM in cell assay.
DMPQ dihydrochloride is a potent and selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ) with an IC50 of 80 nM[1].
NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 0.15 μM, also inhibits InsR, with IC50 of 0.14 μM.
Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting the extracellular domains II and IV of the human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathway. The IgG1 Fc fragment of Anbenitamab binds FcRγIIIa mediates potent antibody dependent cell-mediated cytotoxicity (ADCC) and inhibits tumor cell proliferation. Anbenitamab has the potential for HER2-positive metastatic breast cancer (MBC) research[1][2].
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively[1]. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM[2].
Dilpacimab (ABT165) is a potent dual-variable domain immunoglobulin, targets both delta-like ligand 4 (DLL4) and VEGF pathways.. Dilpacimab can be used in research of cancer[1].
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research[1].
HIV-IN-6 is a HIV-Ⅰ viral replication inhibitor by targeting Src family kinases (SFK) that interact with Nef protein of the virus, such as Hck[1].
Cearoin, isolated from Dalbergia odorifera, increases autophagy and apoptosis through the production of ROS and the activation of ERK[1].
MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.IC50 value:10 nM (VEGFR2), 29 nM(c-Met) [1]Target:VEGFR, c-Metin vivo: MGCD-265-analog has a reasonable half-life, 1.2 h in rats and 5.8 h in dogs, and has an acceptable clearance, 0.33 L/(kg h) in rats and 1.1 L/(kg h) in dogs. The steady state volume of distribution was low in rats (0.25 L/kg) and reasonable in dogs (1.5 L/kg), while the oral bio-availability was determined to be 12% and 42% in rats and dogs, respectively. GCD-265-analog performed well in vivo against a panel of different human tumor types, particularly those that are driven by or overexpress c-Met (MNNGHOS and MKN45). Tumor growth inhibition at a dose of 20 mg/kg po once daily ranged from 41% to 94%. MGCD-265-analog was found to show spill-over inhibition of a number of kinases in addition to the intended c-Met/VEGFR2 activity. MGCD-265-analog has significant antitumor activity in vivo.[1]
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect[1].
Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). Vulinacimab can be used in the research of cancers. VEGFR-2, overexpressed in certain tumors, is critical in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells[1].
EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer[1][2].
GGTI 2417 is the methyl ester prodrug of GGTI-2418, a highly potent, competitive, and selective inhibitor of GGTase I; exhibits potent inhibitory activity against Rap1 geranylgeranylation with IC50 of 400 nM; increases p27 protein levels and induces accumulation in the G0/G1 phase as well as apoptotic cell death in breast cancer cells, and prevents the degradation of nuclear p27.
c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM.c-Fms-IN-10 has anti-tumor activity[1].