Angiogenèse

KRAS G12D inhibitor 25 (Compound 148) acts as an inhibitor for KRAS G12C and HSP90α, displaying IC50 values of <0.1 μM and 0.1-1 μM respectively. Additionally, it suppresses the proliferation of MIA PaCa-2 and NCI-H358 cell lines, with EC50 values of <0.1 μM and 0.1-1 μM correspondingly. This compound also promotes the degradation of ERBB2, exhibiting a DC50 of 0.1-1 μM.

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

Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.

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.

AST5902 is the active metabolite of Alflutinib.

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.

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.

WDR5-47 is a potent small molecule to disturb the interaction of MLL1-WDR5 with IC50 value of 0.3μM.

PROTAC EGFR degrader 4 targets mutant EGFR, degrades del19 and L858R/T790M (DC50: 0.51, 126 nM), and inhibits HCC827, H1975 cell growth (IC50: 0.83, 203.1 nM).

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-15 (compound I-005) is a potent EGFR inhibitor, exhibiting an IC50 value of 4 nM. This compound holds potential for oncological research applications.

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

AG1478 HCl is an epidermal growth factor receptor protein inhibitor.

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

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

Simotinib hydrochloride: selective oral EGFR inhibitor, IC50 19.9 nM, potent anticancer agent.

Mersalyl is an organic mercurial diuretic.

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.