Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 breast cancer, gliomas, et al.
IC50&Target
ADAM10
ADAM17
体外研究
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. Aderbasib (100-1000μM; pre-treated for 0.5 h) shows antiviral effect against CSFV pseudovirus at 100 μM and 1 mM in PK15 cells.
体内研究
Aderbasib (intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks) blocks glioma growth of SU-pcGBM2 NSG mice xenografts. INCB7839 can be formulated in 2% DMSO, 2% Tween 80, 48% PEG300, 48% water as a injection solution. This is for literature reference only.
Animal Model:
NSG mice
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.
分子式
C21H28N4O5
分子量
416.47
CAS号
791828-58-5
运输条件
Room temperature in continental US; may vary elsewhere.