Angiogenèse

TYD-68 is a potent and selective CRBN-recruiting TYK2 PROTAC degrader, with a DC50 value of 0.42 nM. This compound effectively inhibits IL-12 and IFN-α-induced phosphorylation of STAT4 and STAT1, thereby blocking TYK2-dependent signaling pathways. TYD-68 is applicable in psoriasis research.

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.

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

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

SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).

EGFR/HER2/DHFR-IN-2 (Compound 4b) serves as an inhibitor for EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively.

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

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.

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

HER2-IN-13 (Compound 33) serves as an effective HER2 inhibitor, exhibiting an IC50 value of 8 nM, and additionally demonstrates inhibition of wt-EGFR with an

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.

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.

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

MTX-241F, a selective small molecule inhibitor, targets members of the EGFR and PI3 kinase families.

MS9427: PROTAC EGFR degrader, 7.1 nM (WT), 4.3 nM (L858R); targets mutant via UPS and autophagy; inhibits NSCLC cell growth; anticancer research.

JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-cancer.

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

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