Angiogenesis

<p>Potent PROTAC EGFR degrader 2; IC50: 4.0 nM, DC50: 36.51 nM; inhibits cell growth; for NTR-responsive synthesis.</p>

<p>MLK3-IN-1 (Compound 37) is a selective inhibitor of mixed-lineage kinase 3 (MLK3) with an IC50 of less than 1 nM. It also inhibits FAK with an IC50 of 15.5 μM. In both murine and human liver microsomes, MLK3-IN-1 demonstrates excellent metabolic stability.</p>

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

<p>EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.</p>

<p>Syk-IN-4: potent, selective SYK inhibitor, orally bioavailable, IC50=0.31 nM, targets autoimmunity, cancers.</p>

<p>AD57, a polypharmacological agent, blocks RET kinase (IC50: 2 nM), disrupts related kinases, and hinders cancerous activities like invasion and proliferation.</p>

<p>Verucopeptin is a pyranocyclic peptide and HIF-1 inhibitor, an antibiotic effective against B16 melanoma, with anticancer activity.</p>

<p>BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative.</p>

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

<p>Tyrosine kinase substrate peptide</p>

<p>PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET.</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>DSPE-PEG2000-A7R is a PEG compound consisting of DSPE and a tumor vasculature-targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, a receptor that is overexpressed in various tumors.</p>

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

<p>A unique collection of 1353 proangiogenic and antiangiogenic compounds for new targets identification, research in mechanisms of angiogenesis, and high</p>

<p>EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively.</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>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>Emodic acid is a useful organic compound for research related to life sciences. The catalog number is T124807 and the CAS number is 478-45-5.</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>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>VSLRGDTRG is a synthetic peptide derived from the RGD motif in cadherin17 (CDH17) that binds to the α2β1 integrin, activating its signaling pathways. By promoting high-affinity conformational changes in β1 integrins through the RGD motif, VSLRGDTRG enhances cell adhesion and the phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. This peptide is useful for research on cancers expressing CDH17, such as colorectal and pancreatic cancer.</p>

<p>HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM.</p>

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

<p>MY-1576 is a FAK inhibitor with an IC50 of 8 nM. It activates the Hippo pathway, thereby inhibiting YAP/TAZ regulation. Additionally, MY-1576 effectively suppresses tumor growth in the KYSE30 xenograft mouse model, demonstrates good safety, and efficiently downregulates FAK autophosphorylation and YAP/TAZ levels in vivo.</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>AG1478 HCl is an epidermal growth factor receptor protein inhibitor.</p>

<p>SJ10542: potent JAK2/3-targeting PG-PROTAC; DC50s: JAK2 - 14 nM, JAK3 - 11 nM, JAK2-fusion ALL - 24 nM; CRBN recruiter.</p>

<p>Sorafenib D4 is deuterium-labeled Sorafenib, a multi-kinase inhibitor (Raf-1, B-Raf, VEGFR-3) with IC50s: 6, 20, 22 nM.</p>

<p>Bevasiranib is a siRNA targeting VEGF production, key in choroidal neo-vascularization and wet AMD.</p>

<p>MPT0B390 is an inhibitor of HDAC and a TIMP3 inducer inhibiting tumor growth, metastasis, and angiogenesis.</p>

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

<p>DSPE-PEG1000-GE11 is a PEG compound made up of DSPE and an EGFR-targeting peptide (GE11). GE11 is applicable for cancer cells overexpressing EGFR. DSPE-PEG1000-GE11 serves a role in drug delivery.</p>

<p>EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-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>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>DB1113 is a bifunctional kinase degrader, targeting ABL1, ABL2, CDK4, MAPKs, and more for disease research.</p>

<p>GMB-475 is a PROTAC ligand targeting BCR-ABL1 for degradation via E3 ligase recruitment.</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>Arg-IN-1 is a selective covalent inhibitor targeting Arginine (Arg), with IC50 values of 9.7 nM and 30.4 nM for FGFR2 and FGFR3, respectively. This compound is designed to potentially avoid the off-target toxicity of FGFR1/4 and overcome acquired resistance, offering potential in cancer therapies targeting FGFR.</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>AST5902 is the active metabolite of Alflutinib.</p>

<p>DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. It can suppress the proliferation of acute myeloid leukemia cells and induce apoptosis. With its antitumor properties, DD0-2363 is applicable for research on acute myeloid leukemia.</p>

<p>BTK-IN-5 is a covalent inhibitor of Bruton's tyrosine kinase (BTK) designed for the treatment of medical conditions including cardiovascular diseases,</p>

<p>(R)-3-Hydroxy Midostaurin: potent kinase inhibitor, major midostaurin metabolite via CYP3A4, potential AML treatment.</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>DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[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>PF15 TFA, a PROTAC targeting FLT3 kinase and CRBN, exhibits selective degradation of FLT3-ITD with a DC50 of 76.7 nM.</p>

<p>SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.</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>7-Hydroxyneolamellarin A, from Dendrilla nigra, inhibits HIF-1α and VEGF in cancer research.</p>

<p>Istiratumab (M-6495) is a bispecific antibody against IGF-1R/ErbB3 for cancer research, promoting receptor degradation.</p>

<p>SNIPER(ABL)-019, a compound that links Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a</p>

<p>SA-PA, a self-assembled intracellular PROTAC leveraging azide-alkyne click chemistry, selectively degrades VEGFR-2, PDGFR-β, and EphB4 proteins within U87 cells</p>

<p>SNIPER(ABL)-020, a Dasatinib-Bestatin conjugate via linker, inhibits ABL and targets IAP, reducing BCR-ABL protein.</p>

<p>SJF 1521 is an EGFR degrader belonging to the PROTAC class that selectively degrades EGFR while preserving HER2.</p>

<p>ALK/ROS1-IN-5 (compound X4) is a selective inhibitor of ALK and ROS1 kinases, with IC50 values of 0.512 μM for ALK and 0.766 μM for ROS1. It inhibits H2228 cells with an IC50 of 0.034 μM and induces apoptosis in cancer cells in a dose-dependent manner. Additionally, ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells.</p>

<p>AS2553627 is a JAK inhibitor. AS2553627 prevents chronic rejection in rat cardiac allografts.</p>

<p>SJ988497: PROTAC JAK2 degrader, inhibits CRLF2r cell growth, degrades GSPT1, combines Ruxolitinib, linker, Pomalidomide; researched for ALL.</p>

<p>hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX/XII and Vascular Endothelial Growth Factor Receptor 2 (</p>

<p>Bevasiranib sodium, a siRNA, silences genes for VEGF, key in CNV pathogenesis and wet AMD precursor.</p>

<p>PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, promotes Bcr-Abl degradation through the ubiquitin-proteasome pathway and</p>

<p>JAK 3 inhibitor IV (ZM 39923 hydrochloride) is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to</p>

<p>SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein</p>

<p>Sotiburafusp alfa is a humanized bispecific fusion protein comprising a VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) connected</p>

<p>Potent, selective oral PROTAC BTK Degrader-1; IC50: 34.51 nM (WT), 64.56 nM (BTK-481S); reduces BTK protein, inhibits tumors.</p>

<p>EGFR-IN-42 (17b) is a potent EGFR inhibitor with nanomolar efficacy, merging tamoxifen/endoxifen and gefitinib, exhibiting enhanced anti-cancer action.</p>

<p>JH-XI-10-02 selectively degrades CDK8 (IC50: 159 nM) through proteasome, sparing CDK8 mRNA and CDK19.</p>

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

<p>Mal-VC-PAB-(N-Me-amide-C3)-ADU-S100 triethylamine: an ISAC with anti-HER2, STING agonist ADU-S100, linker; for cancer research.</p>

<p>EGFR-IN-86 (compound 4i), an EGFR inhibitor (IC50: 1.5 nM), demonstrates potent activity against glioblastoma by inducing apoptosis and causing G2/M phase cell</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>SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of</p>

<p>Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that shows significant inhibition against a range of protein kinases including RET, KIT,</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>FDU73 is a potent and selective BTK PROTAC degrader with a DC50 of 2.9 nM in JeKo-1 cells. It inhibits tumor cell proliferation and exhibits antitumor activity.</p>

<p>EGFR-IN-140 (Compound 31) is an inhibitor of EGFR, effectively targeting both wild-type EGFR and the EGFRL858R/T790M/C797S mutant, with Ki values of 0.95 nM and 2.1 nM, respectively. Additionally, it inhibits EGFRdel19/T790M/C797S in Ba/F3 cells with an IC50 of 56.9 nM and demonstrates antitumor activity in mouse models.</p>

<p>Varlitinib Tosylate is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2).</p>

<p>EGFR-IN-153 (Compound 5l) is an EGFR inhibitor that suppresses the proliferation of MDA-MB-231 cells with an IC50 of 0.73 μM and induces apoptosis. It is applicable for research in breast cancer.</p>

<p>FAK-IN-27 (compound 8A) is a potent and selective inhibitor of FAK, with an IC50 of 4.968 nM. It effectively inhibits the proliferation of H1299 cells, with an IC50 of 0.28 μM, and is applicable for research in non-small cell lung cancer (NSCLC).</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>Axltide mimics mouse Insulin receptor substrate 1, amino acids 979-989 with sequence KKSRGDYMTMQIG.</p>

<p>SOS1/EGFR-IN-2 (Compound 4) functions as a dual inhibitor of SOS1 and EGFR, exhibiting IC50 values of 8.3 and 14.6 nM, respectively. It demonstrates significant antiproliferative effects on cancer cells harboring various KRAS mutations.</p>

<p>JAK-IN-15 is a JAK inhibitor. WO2016119700A1 (Compound 15).</p>

<p>VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC.</p>

<p>Trastuzumab envedotin (DP303c) is an antibody-drug conjugate (ADC) targeting the human epidermal growth factor receptor 2 (HER2). It consists of the anti-HER2 antibody DP001 linked to the microtubule polymerization inhibitor MonomethylauristatinE (MMAE) through a cleavable linker. This compound is utilized in research involving HER2-positive solid tumors such as breast cancer, colorectal cancer, and gastric cancer.</p>

<p>TL13-112 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.14 nM).</p>

<p>MET/PDGFRA-IN-2 (compound 8h) serves as an inhibitor of MET and PDGFRA proteins, promoting apoptosis in cells and impeding the proliferation of MET-positive</p>

<p>LC-MB12 is a PROTAC FGFR2 compound that degrades FGFR2 and can be used to study gastric cancer.</p>

<p>FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.</p>

<p>Phosphopeptide ligand for the src SH2 domain (IC50 = 1 μM). Blocks src interactions with EGFR and FAK.</p>

<p>K882 (Compound 4e) is an Src inhibitor with a KD of 0.315 μM. It induces apoptosis and inhibits XIAP and Survivin. Additionally, K882 blocks the activation of the PI3K/Akt/mTOR, Jak1/Stat3, and Ras/MAPK signaling pathways. K882 exhibits antitumor activity against non-small cell lung cancer.</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>ML 2-23 is a potent BCR-ABL degrader operating as a PROTAC, exhibiting selective proteasome-dependent degradation of BCR-ABL within leukemia cells [1].</p>

<p>FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.</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>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>Lyso-Monosialoganglioside GM3 (Lyso-GM3) is an analog of Ganglioside GM3 with antitumor properties. It inhibits the increase in EGFR kinase activity induced by EGF in A431 epithelial cancer cells.</p>