Angiogenèse

<p>SPP-037 is an orally active selective inhibitor of ST6GAL1, with an IC50 of 3.59 μM. It exhibits anti-migration activity against MDA-MB-231 cells by inhibiting integrin α2,6-sialylation and the integrin-FAK-paxillin pathway. In MDA-MB-231 xenograft mouse models, SPP-037 demonstrates antitumor properties. This compound is applicable in breast cancer research.</p>

<p>SNIPER(ABL)-044, a compound that links HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a</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>CPD-1224, an oral ALK inhibitor derivative, binds cereblon, targets EML4-ALK fusions, and degrades ALK plus L1196M/G1202R mutants.</p>

<p>Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that effectively impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2.</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>Potent CDK inhibitor 3-Methylthienyl-carbonyl-JNJ-7706621, IC50: CDK1=6.4nM, CDK2=2nM, GSK-3=0.041μM; moderate on CDK4/VEGF-R2/FGF-R2.</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>Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.</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>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>Negative control for TL 13-112 . Displays no degradation of ALK in cell lines. Highly potent ALK inhibitor (IC50 = 0.34 nM).</p>

<p>Simotinib hydrochloride: selective oral EGFR inhibitor, IC50 19.9 nM, potent anticancer agent.</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>Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.</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>GBD-9, a dual-mechanism degrader, effectively promotes the degradation of BTK and GSPT1 through recruitment of E3 ligase cereblon (CRBN).</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>hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide with potential as a dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2.</p>

<p>The compound, Biotin-labeled Syk Kinase Peptide Substrate, is a peptide substrate of Syk kinase that is labeled with biotin.</p>

<p>Potent PROTAC EGFR degrader 3; excellent against H1975/HCC827 cells; lysosome-involved mutant degradation.</p>

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

<p>Inhibits Lyn kinase, blocks IL-5 receptor, prevents eosinophil differentiation and reduces asthma-related inflammation in mice.</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>Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors, has potent antitumor activities.</p>

<p>GMB-475 is a PROTAC ligand targeting BCR-ABL1 for degradation via E3 ligase recruitment.</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>PACAP-38 (31-38), human, mouse, rat (TFA) demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal.</p>

<p>VnP-16 enhances bone formation by stimulating the differentiation and activity of osteoblasts via direct β1 integrin engagement, which subsequently activates</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>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>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>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>MS9427 TFA: PROTAC EGFR degrader, Kd 7.1 nM (WT), 4.3 nM (L858R), targets mutant EGFR, inhibits NSCLC cell growth, for cancer research.</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>Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).</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>