Bafetinib is a Lyn and Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity.
(Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC50s of 6.28 µM and 8.17 µM, respectively[1].
2-Phospho-L-ascorbic acid trisodium salt acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.
Efdamrofusp alfa is a bispecific fusion protein. Efdamrofusp alfa is capable of neutralizing both VEGF isoforms and C3b/C4b. Efdamrofusp alfa can be used for the research of neovascular age-related macular degeneration (nAMD) and other complement-related ocular conditions[1].
Masitinib is an orally available Kit inhibitor with an IC50 of 200 nM. It also inhibits PDGFRα/β with an IC50 of 540 nM/800 nM nM.
GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. GTP-14564 inhibits FLT3 ligand-dependent growth in Ba/F3 leukemia cells[1].
Davutamig (REGN-5093) is a humanized immunoglobulin G4-kappa, anti-MET monoclonal antibody targeting two different nonoverlapping epitopes on MET. Davutamig is an antineoplastic[1].
OSI-296 is a potent and dual inhibitor of cMET and RON kinases (IC50 value are 42 nM and 200 nM for cMet and sfRon respectively) . OSI-206 shows in vivo efficacy and is well tolerated in tumor xenografts models upon oral dosing. OSI-296 also reduces tumour growth in the bone.
KYL peptide is an EphA4 receptor tyrosine kinase inhibitor (Kd=0.8 μM). KYL peptide inhibits EphA4-EphrinA5 interactions (IC50=6.34 μM). KYL peptide prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. KYL peptide also exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively).
ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation[1].
Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline nitrate can be used for non-bacterial conjunctivitis research[1][2].
GNF2133 is a selective DYRK1A inhibitor with an IC50 value of 6 nM.
Mecasermin (Human IGF-I; FK 780) is a recombinant human insulin-like growth factor I (IGF-I). Mecasermin has the potential for the study of the growth failure of growth hormone (GH) insensitivity caused by GH receptor defects or GH-inhibiting antibodies[1].
FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively[1].
CCT 365623 (CCT365623) hydrochloride is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM; inhibits LOX actvity in living cell system (MDCK cysts) at 5 uM, reduces EGFR retention at the cell surface, suppresses EGFR and AKT phosphorylation driven by EGF, also activates SMAD2 and downregulates MATN2; delays the growth of primary and metastatic tumour cells in vivo.
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research[1][2].
CH7057288 is a potent and selective TRK inhibitor.
DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
Eflapegrastim is a humanized IgG4 monoclonal antibody, is also a granulocyte colony-stimulating factor (G-CSF). Eflapegrastim targets to G-CSF receptor (c-Fms). Eflapegrastim stimulates proliferation and differentiation of neutrophil progenitor cells and maintains stable numbers of mature and functional neutrophils. Eflapegrastim also shortens the duration of neutropenia[1].
(E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor[1].
FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively; FN-1501 has anticancer activity.
Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent monomethyl auristatin E. Disitamab vedotin enhances antitumor immunity[1].
Epidermal Growth Factor Receptor Peptide (985-996) is an amino acid peptide fragment derived from positions 985-996 in epidermal growth factor receptor (EGFR)[1].
ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degrading molecule. ITK degrader 2 degrades ITK[1].
PROTAC EGFR degrader 6 (Compound 2), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].
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].
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.
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].
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].