Angiogenesis

<p>Apoptosisinducer 35 (Compound 6) is a multi-target inhibitor that reduces the expression of EGFR, AKT, ERK, and P38-MAPKα. It suppresses the proliferation of cancer cells A549 and Jurkat, induces cell cycle arrest at the S phase, and triggers apoptosis (cell death).</p>

<p>Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors, has potent antitumor activities.</p>

<p>TL13-12 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.69 nM).</p>

<p>JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively).</p>

<p>SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.</p>

<p>PTD10, a highly potent PROTAC BTK degrader, exhibits a DC50 of 0.5 nM and a KD of 2.28 nM.</p>

<p>EGFR-IN-22: potent for EGFR (IC50: 4.91 nM) &amp; L858R/T790M/C797S mutation (IC50: 0.54 nM).</p>

<p>SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker.</p>

<p>2-Keto Crizotinib is an active lactam metabolite of crizotinib.</p>

<p>KIT/PDGFRA-IN-1 (compound 19) is an inhibitor targeting the stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA). Its IC50 values are 2.3 µM for KIT-wt, 12 µM for KIT-D816H, 492 µM for KIT-T670I, 0.8 µM for PDGFRA-wt, 99.9 µM for PDGFRA-D842V, 42.3 µM for PDGFRA-T674I, and 4.3 µM for PDGFRA-G680R. The GR50 values for GIST-T1, T1-a-D842V, and GIST-48B cell lines (gastrointestinal stromal tumor cell lines with PDGFR and KIT mutations) are 12 nM, 8900 nM, and ≥10,000 nM, respectively.</p>

<p>Cetuximab (PBS) is a human IgG1 monoclonal antibody that inhibits the epidermal growth factor receptor (EGFR), with a dissociation constant (Kd) of 0.201 nM for EGFR as measured by the SPR method. It exhibits potent antitumor activity.</p>

<p>Zilurgisertib (INCB-000928) is a selective and potent ALK 2 inhibitor for the study of cancer and MF anemia.</p>

<p>A unique collection of 1336 HIF-1 related small chemicals can be used for drug discovery in ischemic disease and cancer and related mechanism studies；</p>

<p>SNIPER(ABL)-033, a compound that conjugates HG-7-85-01 (ABL inhibitor) to a LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein</p>

<p>PROTAC FGFR1 degrader-1 (compound S2H) is a targeted degrader of FGFR1, demonstrating an IC50 of 26.81 nM and a DC50 of 39.78 nM in KG1a cells. This compound is composed of a CRBN-type E3 ligase ligand (blue part) Pomalidomide, a target protein ligand (red part) FGFR1ligand-1, and a PROTAC linker (black part) 9-Bromononanoic acid, together forming the conjugate E3LigaseLigand-linker Conjugate 164.</p>

<p>CEP-5214: Powerful pan VEGF-R tyrosine kinase inhibitor; IC50: 16nM (R1), 8nM (R2), 4nM (R3); effective in cells.</p>

<p>Si5-N14 is a key component of siloxane-linked lipid nanoparticles (SiLNP) with properties that enhance vascular repair and exhibit antitumor activity. In transgenic GFP mouse models, Si5-N14 mediates CRISPR-Cas9 editing. In Lewis lung carcinoma (LLC) tumor mouse models, it leads to the knockdown of vascular endothelial growth factor receptor 2 (VEGFR2), producing antitumor effects. Additionally, in mice with virus-induced lung injury, Si5-N14 facilitates the delivery of fibroblast growth factor-2 (FGF-2) mRNA, promoting vascular repair, oxygenation, and improved lung function. Si5-N14 shows potential for research in tumors, pneumonia, and cardiovascular diseases.</p>

<p>PROTAC EGFR degrader 4 targets mutant EGFR, degrades del19 and L858R/T790M (DC50: 0.51, 126 nM), and inhibits HCC827, H1975 cell growth (IC50: 0.83, 203.1 nM).</p>

<p>ALK-IN-9 effectively inhibits cell growth with IC50 &lt;0.2 nM for Ba/F3-EML4-ALK, KM12, KG-1.</p>

<p>TYK2activator-1 (16b) is a TYK2 activator with an EC50 value of 1.78 μM. It inhibits JAK2 and JAK3 with IC50 values of 6.8 μM and 6.3 μM, respectively.</p>

<p>PM-8002 is a bispecific antibody that targets PD-L1 and VEGF-A. It is applicable for research on solid tumors.</p>

<p>OK2, a specific inhibitor of the CCN2/EGFR interaction, effectively disrupts this interaction by binding to the CT domain of CCN2.</p>

<p>SNIPER(ABL)-015, a compound that conjugates GNF5 (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of 5</p>

<p>PF15 TFA, a PROTAC targeting FLT3 kinase and CRBN, exhibits selective degradation of FLT3-ITD with a DC50 of 76.7 nM.</p>

<p>VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.</p>

<p>EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer.</p>

<p>Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values</p>

<p>Axltide mimics mouse Insulin receptor substrate 1, amino acids 979-989 with sequence KKSRGDYMTMQIG.</p>

<p>Phage display selected Affibody ligands for HER2/neu from a protein library based on a 58-residue Staphylococcal protein A Z domain.</p>

<p>Duligotuzumab is a dual-targeting anti-EGFR/HER3 mAb that blocks signaling and induces ADCC for tumors with poor prognosis.</p>

<p>EGFR-IN-144 (Compound 4B) inhibits EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). It exhibits cytotoxicity in various cancer cells with a GI50 at the nanomolar level. EGFR-IN-144 reduces the expression of mTOR, TNF-α, and IL-6, causes G1/S phase cell cycle arrest, and induces apoptosis.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>MP-RM-1 is a selective murine monoclonal antibody inhibitor that targets the human epidermal growth factor receptor 3 (ErbB-3). It blocks ErbB-3 activation induced by neuregulin 1 (NRG-1β), facilitates ErbB-3 internalization and degradation, and inhibits downstream signaling pathways like PI3K-Akt. MP-RM-1 shows potential for research on ErbB-3-overexpressing solid tumors such as breast cancer, melanoma, and prostate cancer.</p>

<p>EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.</p>

<p>ALK-IN-13 is an ALK inhibitor.</p>

<p>BW710 is an orally active inhibitor specifically targeting fibroblast growth factor receptor 2 (FGFR2). It effectively inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 2.8 nM. BW710 completely suppresses FGFR2 enzymatic activity and demonstrates selectivity among 75 tyrosine kinases, including FGFR1, FGFR3, and FGFR4, at a 1 μM concentration. Additionally, BW710 impedes FGFR2 signaling and selectively inhibits the proliferation of cancer cells driven by FGFR2. It exhibits promising pharmacokinetic properties, with an oral bioavailability of 29% in mice.</p>

<p>Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).</p>

<p>MS9427: PROTAC EGFR degrader, 7.1 nM (WT), 4.3 nM (L858R); targets mutant via UPS and autophagy; inhibits NSCLC cell growth; anticancer research.</p>

<p>DSPE-PEG5000-A7R is a PEG compound composed of DSPE and the tumor vascular targeting peptide (A7R). The peptide A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors.</p>

<p>AD57 is a potent inhibitor of both c-Src and Abl with IC50 of 0.025 μM and 0.041 μM, respectively.</p>

<p>AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.</p>

<p>BTK inhibitor 19 is a highly selective, covalent BTK inhibitor ( IC 50 = 2.7 nM).</p>

<p>EGFR-IN-83 (Compound 9), an EGFR inhibitor with an IC50 of 2.53 nM, exhibits antiproliferative effects on MCF-7 and MDA-MB-231 cell lines, with respective IC50</p>

<p>ALK protein ligand-1 (Compound A1) is an ALK protein ligand, acting as a ligand for the target protein in PROTACs, demonstrating inhibitory effects on ALK. It is also useful in the synthesis of AP-1.</p>

<p>Trastuzumab emtansine is a HER2-targeted ADC for advanced breast cancer, combining trastuzumab with DM1 cytotoxicity.</p>

<p>LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR, with IC50 values of 71.6 nM and 8.9 nM, respectively. It blocks FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation, and also inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). Furthermore, LC-SF-14 exhibits antitumor activity in SNU-16 xenograft mouse models, making it suitable for research on FGFR2-driven gastric cancer.</p>

<p>FLT3/VEGFR2-IN-1 (Compound 26) is a potent inhibitor of FLT3, VEGFR2, and HDAC, exhibiting IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM against FLT3, VEGFR2, and HDAC1, respectively. It effectively inhibits the phosphorylation of STAT3 and ERK1/2, as well as the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 demonstrates antitumor activity and is applicable in research on acute myeloid leukemia.</p>

<p>DSPE-PEG5000-GE11 is a PEG compound composed of DSPE and the EGFR-targeting peptide (GE11). GE11 is applicable for cancer cells with EGFR overexpression. DSPE-PEG5000-GE11 is utilized in drug delivery.</p>

<p>AXL/Angiokinase-IN-1 (compound 11b) is an inhibitor of AXL/triple angiokinase, with an IC50 of 3.75 nM for AXL expression. This compound suppresses epithelial-mesenchymal transition (EMT) in Bxpc-3 cells and prevents metastasis in lung cancer cells. Additionally, AXL/Angiokinase-IN-1 impairs the functions of vascular and fibroblast cells and induces apoptosis in both cancer and fibroblast cells. It is characterized by low toxicity and favorable metabolic stability.</p>

<p>BTKligand-14 is a PROTAC-targeting ligand for BTK, suitable for the synthesis of FDU73.</p>