Angiogenèse

MS9449 is a powerful EGFR PROTAC; Kd: 17 nM (WT), 10 nM (L858R); targets mutant EGFRs via UPS and autophagy; hinders NSCLC cell growth.

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

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,

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

CG-3-246 is a dual inhibitor targeting FLT3 and BCL-2, with dissociation constants (Kd) of 63 nM and 4.25 nM, respectively. This compound plays a significant role in acute myeloid leukemia research.

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.

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

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

Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-VEGFR-2.

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

(R)-3-Hydroxy Midostaurin: potent kinase inhibitor, major midostaurin metabolite via CYP3A4, potential AML treatment.

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

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.

PROTAC VEGFR-2 degrader-1 shows minimal VEGFR-2 inhibition & low anti-proliferative effect on EA.hy926 cells.

DBL-6-13 is an inhibitor of WDR5, displaying moderate binding affinity with dissociation constants (Kd) of 6.8 μM and 9.1 μM as determined by microscale thermophoresis analysis and fluorescence polarization analysis, respectively.

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values

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

ZM 449829: Selective JAK3 inhibitor, binds to ATP site. pIC50: 6.8 for JAK3, others < 5.0.

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

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].

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.

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

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.

dALK-3 is a degrader of anaplastic lymphoma kinase (ALK) that effectively induces the degradation of EML4-ALK with a DC50 of 0.182 μM. It exhibits significant antiproliferative activity against H3122 cells and is applicable for tumor research.

Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.

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.

HAT-SIL-TG-1&AT: a hypoxia-activated JAK inhibitor that curbs HEL cell growth & STAT3/5 phosphorylation in tumors.

WYE-687 is a selective mTOR inhibitor (IC50: 7 nM), over 100x more selective for mTOR than PI3Kα/γ, affecting mTORC1/pS6K and mTORC2/P-AKT(S473).

ALK-IN-29 (compound 4c) exhibits inhibitory effects on tyrosine protein kinases such as ALK, CDK2/CyclinE1, and FAK, with the strongest inhibition observed against ALK kinase, displaying a 40.63% inhibition rate at a concentration of 10 μM. ALK-IN-29 is applicable in cancer research.

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].

EGFR-IN-84 (Compound 6g), an EGFR inhibitor with an IC50 of 24 nM, impedes the growth of A549 cells with an IC50 value of 1.537 μM and is utilized for lung

FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.

AG1478 HCl is an epidermal growth factor receptor protein inhibitor.

FGFR1 inhibitor-2, potent at 4.55 μM IC50 in MDA-MB-231, targets triple-negative breast cancer.

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

Mersalyl is an organic mercurial diuretic.

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

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.

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.

WAY-270250 is an IGF-1R/SRC inhibitor.

VEGFR-2-IN-59 (Compound 3h) is an inhibitor of VEGFR2 with an IC50 of 3.73 µM. It exhibits cytotoxicity in cancer cell lines A549, HT-29, A375, MCF7, and NHDF, with IC50 values of 20.91, 19.70, 9.63, 17.43, and 20.71 μM, respectively. VEGFR-2-IN-59 also inhibits tubular structure formation and demonstrates anti-angiogenic properties.

Befotertinib (D-0316) is an inhibitor of EGFR tyrosine kinase and can be used for studies about EGFR T790M-positive non-small cell lung cancer.

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

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.

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

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.

Ibrutinib-biotin probe links Ibrutinib to biotin, with IC50 0.755-1.02 nM for BTK (patent WO2014059368A1).

EGFR/VEGFR2-IN-1 (Compound 10e) serves as an inhibitor for VEGFR-2 and EGFR, with respective IC50 values of 0.26 and 0.14 μM. It inhibits microtubule protein polymerization with an IC50 of 40.9 μM and induces cell apoptosis (Apoptosis). EGFR/VEGFR2-IN-1 is applicable in research related to anti-leukemia and anti-lymphoma treatments.

Erlotinib-13C6 (CP-358774-13C6), a 13C-labeled direct EGFR inhibitor, IC50: 2 nM.

BRK inhibitor P21d HCl targets breast tumor kinase with 30 nM IC50, suppresses p-SAM68 at 52 nM, useful for in vivo breast cancer research.

EGFR-IN-116 (compound 14D) is an antineoplastic agent. It exhibits an IC50 value of 0.103 μM for EGFR, 0.069 μM for VEGFR-2, and 19.74 μM for Topo II.

MR44397 is a ligand for WD40 repeat (WDR) 5 and is applicable in cancer research.

FAK-IN-9 (8f) is a potent oral FAK inhibitor, IC50 of 27.44 nM; induces TNBC cell apoptosis.

PROTAC BTK Degrader-6 (Compound 15), with a DC50 of 3.18 nM, exhibits anti-inflammatory properties by inhibiting NF-κB activation and suppressing the expression

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

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

SNIPER(ABL)-013, a compound that links GNF5 (ABL inhibitor) with Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of

VnP-16 enhances bone formation by stimulating the differentiation and activity of osteoblasts via direct β1 integrin engagement, which subsequently activates

PF15 TFA, a PROTAC targeting FLT3 kinase and CRBN, exhibits selective degradation of FLT3-ITD with a DC50 of 76.7 nM.

EGFR-IN-43 (17c) is a potent EGFR inhibitor with ER antagonist action, tamoxifen/endoxifen+gefitinib linkage, and strong anticancer activity.

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.

FLT3-IN-22 (compound 22f) is a potent inhibitor of FLT3, demonstrating IC50 values of 0.941 nM for FLT3 and 0.199 nM for the FLT3/D835Y mutant.

MS9427 TFA: PROTAC EGFR degrader, Kd 7.1 nM (WT), 4.3 nM (L858R), targets mutant EGFR, inhibits NSCLC cell growth, for cancer research.

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.

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.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM).

PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET.

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.

VEGFR-2-IN-56 (compound 12e) exhibits the strongest inhibition activity against VEGFR-2, with an IC50 value of 45.9 nM.

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 (

ZSH-2117 is a covalent and selective EGFR PROTAC degrader, with a DC50 of 45 nM in Ba/F3-EGFR[L858R/T790M/C797S] cells. It significantly inhibits cell proliferation and reduces AKT and ERK protein levels in downstream EGFR signaling pathways. ZSH-2117 effectively suppresses tumor growth in Ba/F3-EGFR[L858R/T790M/C797S] xenograft mouse models.

CPD-1224, an oral ALK inhibitor derivative, binds cereblon, targets EML4-ALK fusions, and degrades ALK plus L1196M/G1202R mutants.

FLT3-IN-23 (compound 15), a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3), exhibits an IC 50 value of 7.42 nM and demonstrates antiproliferative effects

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.

WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor targeting EGFR and CDK-2, demonstrating IC50 values of 89.6 nM for EGFR and 165.4 nM for CDK-2.

SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.

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

PROTAC EGF Rdegrader 10 (Compound B56) is a PROTAC degrader targeting the epidermal growth factor receptor (EGFR) with a DC50 of less than 100 nM. It binds to CRBN-DDB1 with a Ki of 37 nM and degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibiting the proliferation of BaF3 wild-type and EGFR mutants with an IC50 of less than 150 nM.

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.

7-Hydroxyneolamellarin A, from Dendrilla nigra, inhibits HIF-1α and VEGF in cancer research.

Candidalysin is a cytolytic peptide toxin initially isolated from *Candida albicans*, exhibiting both toxic and non-toxic properties. It activates epithelial cell signaling pathways by interacting with the epithelial growth factor receptor (EGFR) on host cells, leading to the activation of matrix metalloproteinases (MMP) and calcium ion influx, which results in inflammatory responses and immune cell recruitment. Additionally, Candidalysin exhibits cytotoxicity by causing membrane damage to host cells.

ALK-IN-12: potent ALK inhibitor (IC50: 0.18 nM), affects IGF1R and InsR (IC50: 20.3/90.6 nM), potential for cancer therapy.

Anti-FLT3 Antibody (AGS62P) is an ADC antibody targeting FLT3 for research in acute myeloid leukemia.

Phage display selected Affibody ligands for HER2/neu from a protein library based on a 58-residue Staphylococcal protein A Z domain.

EGFR T790M/L858R-IN-6 (compound 53), classified as a pyrimidine compound, serves as an effective inhibitor of EGFR T790M/L858R, demonstrating 90.88% inhibition of enzyme activity at a concentration of 0.05 μM [1].

VEGFR-2/InhA-IN-1, a dual inhibitor based on pyrazole, targets InhA and VEGFR, exhibiting both anti-tuberculosis and anti-angiogenic properties. It demonstrates effective antibacterial activity against the Mycobacterium tuberculosis H37Rv strain (MIC = 6.25 μg/mL) and significantly suppresses VEGFR-2 activity (IC 50 = 15.27 nM).

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.

DC-Srci-6649 is a potent and selective inhibitor of c-Src kinase, effectively blocking its phosphorylation and stabilizing it in an inactive conformation.

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

TX2-120-1 possesses the ability to bind with Her3, exhibiting an IC50 of 56 nM for Her3. It can be utilized in the synthesis of TX2-121-1.

AST5902 is the active metabolite of Alflutinib.

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.

GMB-475 is a PROTAC ligand targeting BCR-ABL1 for degradation via E3 ligase recruitment.

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.

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.