Aderbasib (INCB007839) is a highly potent and orally active hydroxamate-based inhibitor of ADAM10 and ADAM17, with low nanomolar affinity. This compound demonstrates strong antineoplastic activity and holds potential for cancer research in various areas, such as diffuse large B-cell non-Hodgkin lymphoma, HER2-positive breast cancer, gliomas, and more.

Aderbasib inhibits the metalloprotease activity through binding to the active site of the metalloproteinase domain. Aderbasib (10-100 μM) inhibits the interaction between ADAM17 and sE2-Fc, as the concentration of the compound increases, binding of sE2-Fc decreased accordingly, with almost no binding detected at 100 μM in trypsinized PK15 cells[2].Aderbasib (100-1000μM; pre-treated for 0.5 h) shows antiviral effect against CSFV pseudovirus at 100 μM and 1 mM in PK15 cells[2].

Aderbasib (intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks) blocks glioma growth of SU-pcGBM2 NSG mice xenografts[1].INCB7839 can be formulated in 2% DMSO, 2% Tween 80, 48% PEG300, 48% water as a injection solution. This is for literature reference only[1]. Animal Model: NSG mice[1]Dosage: 50 mg/kg Administration: Intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks Result: Robustly inhibited growth of pediatric glioblastoma orthotopic xenografts.