Aderbasib T40901

Product Introduction
Bioactivity


英文名: Aderbasib

描述: 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.

体外活性: 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].

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: INCB 7839 | INCB 007839 | INCB-007839 | Aderbasib | INCB-7839

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途