Angiogenesi

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>Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and</p>

<p>Compound Rh2 (Anticancer agent 133) is a cytotoxic and antimetastatic agent that induces cell cycle arrest, apoptosis, and autophagy.</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>

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.

Tyrosine kinase substrate peptide

<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>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>PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.</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.

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.

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>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>

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.

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

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

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

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>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>

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.

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

<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>EGFR-IN-162 (compound 20) is an effective EGFR inhibitor that enhances both early and late apoptosis (EGFR) as well as necrosis (necrosis). It shows potential for use in breast cancer research.</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>

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>PROTAC EGFR degrader 6 effectively degrades EGFR Del19 in HCC827 cells (DC50=45.2 nM) and induces apoptosis and G1 arrest.</p>

Amuvatinib HCl (MP470 HCl) is a multi-targeted oral tyrosine kinase inhibitor and hinders RAD51-mediated DNA repair, exhibiting anticancer properties.

<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>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>Anti-ERBB3/HER3 (29Z6) is an antibody inhibitor targeting human ERBB3/HER3.</p>

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

Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in

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

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).

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>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>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>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>

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.

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.

PACAP-38 (31-38), human, mouse, rat (TFA) demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal.

<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>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>

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.

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>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>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>

Mersalyl is an organic mercurial diuretic.