Angiogenèse

<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>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>BV02 blocks 14-3-3 interactions, useful in chronic myeloid leukemia research, targets T315I mutant and wild-type Bcr-Abl cells.</p>

<p>MHES0488A is a selective humanized antibody targeting HER2, with a KD value of 0.8 nM. It constitutes the antibody portion of DHES0815A. Upon cellular internalization, MHES0488A is transported to lysosomes, releasing PBD-monoamide into the nucleus, where it alkylates DNA, inducing DNA damage and apoptosis. It shows potential for research in cancers such as HER2-positive breast cancer and gastric cancer.</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>Ibrutinib-biotin probe links Ibrutinib to biotin, with IC50 0.755-1.02 nM for BTK (patent WO2014059368A1).</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>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>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>ALK-IN-9 effectively inhibits cell growth with IC50 &lt;0.2 nM for Ba/F3-EML4-ALK, KM12, KG-1.</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>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>DSPE-PEG2000-GE11 is a PEG compound composed of DSPE and an EGFR-targeting peptide (GE11). GE11 is applicable for cancer cells that overexpress EGFR. DSPE-PEG2000-GE11 is utilized in drug delivery.</p>

<p>Duligotuzumab is a dual-targeting anti-EGFR/HER3 mAb that blocks signaling and induces ADCC for tumors with poor prognosis.</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>Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.</p>

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

<p>Potent BTK Degrader, IC50=5.1nM, CRBN-dependent, suppresses MCL; degrades Ibrutinib-resistant BTK, no kinases binding, reduces tumors in models.</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>

<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>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>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>SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).</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>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>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>LC-MB12 is a PROTAC FGFR2 compound that degrades FGFR2 and can be used to study gastric cancer.</p>

<p>Anti-ERBB3/HER3 (29Z6) is an antibody inhibitor targeting human ERBB3/HER3.</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>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>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>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>BTK inhibitor 19 is a highly selective, covalent BTK inhibitor ( IC 50 = 2.7 nM).</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>SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.</p>

<p>TL13-112 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.14 nM).</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>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>Hck-IN-2 (Compound 8e) acts as an HCK inhibitor with demonstrated cytotoxic effects on tumor cells. It exhibits an IC50 of 19.58 μM for MDA-MB231 cells and 1.42 μM for MCF-7 cells. Additionally, Hck-IN-2 possesses antitumor activity.</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>PACAP-38 (31-38), human, mouse, rat (TFA) demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal.</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>HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases.</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>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>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>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>