Angiogenesis

<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>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>VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively.</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>

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

<p>PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production</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>PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM).</p>

<p>SJF620 hydrochloride is a PROTAC that utilizes a lenalidomide analog to recruit CRBN and ligands to target Btk, exhibiting a DC50 of 7.9 nM [1].</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>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>PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET.</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>TLT8 is a ByeTAC protein degrader that targets BTK. It induces BTK degradation by non-covalently binding to Rpn-13 and BTK. TLT8 is applicable in research on chronic lymphocytic leukemia.</p>

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

<p>EGFR-TK-IN-5 (Compound NCE 2) is a thiazolyl pyrazoline derivative with significant inhibitory activity and stability against EGFR. It is applicable in tumor research.</p>

<p>PROTAC EGFR degrader 6 effectively degrades EGFR Del19 in HCC827 cells (DC50=45.2 nM) and induces apoptosis and G1 arrest.</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-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>SNIPER(ABL)-020, a Dasatinib-Bestatin conjugate via linker, inhibits ABL and targets IAP, reducing BCR-ABL protein.</p>

<p>Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.</p>

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

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

<p>HAT-SIL-TG-1&amp;AT: a hypoxia-activated JAK inhibitor that curbs HEL cell growth &amp; STAT3/5 phosphorylation in tumors.</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>Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.</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>Duligotuzumab is a dual-targeting anti-EGFR/HER3 mAb that blocks signaling and induces ADCC for tumors with poor prognosis.</p>

<p>SJ988497: PROTAC JAK2 degrader, inhibits CRLF2r cell growth, degrades GSPT1, combines Ruxolitinib, linker, Pomalidomide; researched for ALL.</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>(R)-3-Hydroxy Midostaurin: potent kinase inhibitor, major midostaurin metabolite via CYP3A4, potential AML treatment.</p>

<p>Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.</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>WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.</p>

<p>EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.</p>

<p>JAK1/STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1/STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1/STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1/JAK1 and p-STAT3/STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).</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>BTK degrader-1 (compound 1), a bifunctional degrader of Bruton's tyrosine kinase (BTK), demonstrates the capability to be conjugated with CD79b and exhibits anti-tumor effects [1].</p>

<p>Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor active against VEGFR2, EGFR, HER2, and CDK2, with respective IC50 values of 0.33, 0.22, 0.</p>

<p>EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2, exhibiting an IC50 value of 1.15 µM for VEGFR2 and 0.28 µM for EGFRT790M. This compound demonstrates significant anticancer activity.</p>

<p>EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. It effectively suppresses the proliferation of various lung cancer cells, with IC50 values of 11.7, 5.19, 7.32, and 1.53 μM for NCI-H1781, HCC827, NCI-H3255, and NCI-H1975, respectively. Additionally, EGFR-IN-151 hinders colony formation and cell migration in H1975, induces G1 phase cell cycle arrest, and triggers apoptosis in H1975 cells.</p>

<p>FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.</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>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>OK2, a specific inhibitor of the CCN2/EGFR interaction, effectively disrupts this interaction by binding to the CT domain of CCN2.</p>

<p>Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.</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>Phosphopeptide ligand for the src SH2 domain (IC50 = 1 μM). Blocks src interactions with EGFR and FAK.</p>

<p>SC209, a STRO-002 metabolite from patent WO2021247798, synthesizes anti-EGFR ADCs.</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>EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual inhibitor of EGFR and BRAFV600E, with IC50 values of 61 nM and 43 nM, respectively. It halts the cell cycle, induces apoptosis in both early and late stages, and inhibits cancer cell growth in vitro, showing broad-spectrum anticancer activity.</p>

<p>GBD-9, a dual-mechanism degrader, effectively promotes the degradation of BTK and GSPT1 through recruitment of E3 ligase cereblon (CRBN).</p>

<p>MC-Val-Cit-PAB-Amide-TLR7 agonist 4 Conjugate is a conjugate formed by linking MC-Val-Cit-PAB-Amide and TLR7 agonist 4, useful for cancer research.</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>ML228 activates HIF pathway and VEGF, with EC50 of 1μM, effective in vitro.</p>

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

<p>Amuvatinib HCl (MP470 HCl) is a multi-targeted oral tyrosine kinase inhibitor and hinders RAD51-mediated DNA repair, exhibiting anticancer properties.</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>Verucopeptin is a pyranocyclic peptide and HIF-1 inhibitor, an antibiotic effective against B16 melanoma, with anticancer activity.</p>

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

<p>YH32367 (ABL105) is a bispecific antibody targeting HER2 and 4-1BB. It induces the secretion of IFN-γ, resulting in the death of tumor cells when co-cultured with hPBMC and HER2-expressing tumor cells. YH32367 demonstrates notable antitumor activity.</p>

<p>Syk signaling is key in lupus. Syk inhibitors reduce inflammation and sepsis severity in FcgRIIb-/- mice, lowering cytokines and organ damage.</p>

<p>Negative control for TL 13-112 . Displays no degradation of ALK in cell lines. Highly potent ALK inhibitor (IC50 = 0.34 nM).</p>

<p>Zeteletinib hemiadipate (BOS-172738; DS-5010) is an oral RET kinase blocker with nanomolar potency and strong anti-tumor properties.</p>

<p>PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells.</p>

<p>DSPE-PEG1000-A7R is a PEG compound consisting of DSPE and the tumor vasculature-targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors.</p>

<p>Anticanceragent 271 (compound 5C) exhibits antiproliferative activity against lung cancer (A549), colon cancer (Caco-2) cell lines, and human lung fibroblasts (WI38), with an IC50 value of 9.18 μM for A549 cells. This compound can downregulate PI3K and mTOR gene expression and is applicable in cancer research.</p>

<p>DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[1].</p>

<p>MTX-241F, a selective small molecule inhibitor, targets members of the EGFR and PI3 kinase families.</p>

<p>BTK inhibitor 19 is a highly selective, covalent BTK inhibitor ( IC 50 = 2.7 nM).</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>PST3.1a is a selective inhibitor of Mannoside acetyl glucosaminyltransferase 5 (MGAT5), used for studying glioblastoma multiforme (GBM). PST3.1a inhibits TGF-βR and FAK signalling associated with doublecortin (DCX), increases OLIG2 expression, and suppresses the invasion and proliferation of GBM initiator cells (GICs).</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>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>EGFR/HER2/DHFR-IN-2 (Compound 4b) serves as an inhibitor for EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively.</p>

<p>EGFR-IN-120 (Compound 11eg) is an orally effective EGFR inhibitor. It exhibits potency against the EGFR L858R/T790M/C797S mutant with an IC50 of 0.053 μM, and displays weaker activity against EGFRWT, with an IC50 of 1.05 μM. EGFR-IN-120 inhibits the phosphorylation of EGFR as well as key downstream effectors including STAT3, AKT, and Erk. This compound induces cell cycle arrest and apoptosis in cells harboring the EGFR mutation. Additionally, EGFR-IN-120 inhibits the proliferation of NSCLC cells containing the EGFR L858R/T790M/C797S mutation, with an IC50 value of 0.052 μM.</p>

<p>Inhibits Lyn kinase, blocks IL-5 receptor, prevents eosinophil differentiation and reduces asthma-related inflammation in mice.</p>

<p>Varlitinib Tosylate is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2).</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>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>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>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>COVA208 is a bispecific FynomAb targeting HER2, consisting of a fusion protein of an antibody and a FynSH3-derived binding protein. It induces the degradation of HER2, reducing the levels of HER2, HER3, and EGFR, effectively blocking downstream signaling pathways such as HER3-PI3K-AKT and MAPK, and inducing apoptosis in tumor cells. COVA208 shows promise for research in cancers like HER2-positive breast, gastric, and colorectal cancers.</p>

<p>hCA/VEGFR-2-IN-4 (compound 15b), an indolinylbenzenesulfonamide, serves as a potential dual inhibitor targeting cancer-related human carbonic anhydrases hCA IX/</p>

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

<p>Mersalyl is an organic mercurial diuretic.</p>

<p>EGFR/CDK2-IN-3 (compound 4b) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 71.7 nM and 113.7 nM, respectively.</p>

<p>IOX2-NH2-Methyl is a modified form of IOX2. IOX2 is a specific inhibitor of PHD2 (prolyl-hydroxylase-2), capable of upregulating HIF-1α expression and suppressing ROS production. IOX2-NH2-Methyl is employed in investigations of platelet and thrombus formation.</p>

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

<p>Antifibrotic agent 1 is an orally active medication designed to treat idiopathic pulmonary fibrosis (IPF). It effectively mitigates IPF-related processes, including TGF-β-induced epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), as well as profibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α, and Src family kinases (SFKs), while sparing VEGFR, FGFR, and Abl to minimize off-target toxicity. In a bleomycin (BLM)-induced pulmonary fibrosis mouse model, it demonstrates strong antifibrotic activity.</p>

<p>SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells.</p>

<p>IBI-334 is a bispecific antibody targeting both B7-H3 and EGFR. It features an EGFR arm responsible for signal blocking, connected to a modified B7-H3 arm that ensures optimal affinity and binding. The antibody is afucosylated to enhance its antibody-dependent cellular cytotoxicity (ADCC) effects. IBI-334 is widely applicable in EGFR-driven solid tumors.</p>

<p>SJ1008030 (compound 8) formic is a selective JAK2 degrader within the PROTAC class, demonstrating efficacy in inhibiting MHH-CALL-4 leukemia cell growth with an</p>

<p>IMC-D11 (LY-3076226 antibody) is an IgG1 monoclonal antibody targeting FGFR3. It serves as the antibody component of LY3076226. For its isotype control, refer to Human IgG1 kappa, Isotype Control.</p>

<p>E-7090 is a fibroblast growth factor receptor inhibitor. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3.</p>

<p>AMX-818 is a conditionally activated, masked T cell engager (TCE) that targets HER2. It demonstrates potent T cell cytotoxicity against HER2-positive tumor cell lines and can induce tumor regression in vivo. AMX-818 holds promise for research into HER2-positive solid tumors.</p>

<p>ABP-102 (CT P72) is a bispecific t-cell adduct (BiTE) that acts as a CD3 modulator and selective HER2 modulator for targeting HER2 overexpressing tumors.</p>

<p>JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations.</p>