Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Description | 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. |
In vitro | Aderbasib acts by inhibiting metalloprotease activity, specifically binding to the active site within the metalloproteinase domain. At concentrations ranging from 10-100 μM, Aderbasib reduces the interaction between ADAM17 and sE2-Fc; notably, this interaction decreases as Aderbasib concentration increases, leading to a substantial reduction in sE2-Fc binding at 100 μM in trypsinized PK15 cells[2]. Additionally, when pre-treated for 0.5 h, Aderbasib displays an antiviral effect against CSFV pseudovirus at both 100 μM and 1 mM concentrations in PK15 cells[2]. |
In vivo | Aderbasib (intraperitoneal injection; 50 mg/kg; 5 days per week for 2 weeks starting from the fourth week) effectively inhibits the growth of glioma in SU-pcGBM2 NSG mouse xenografts[1]. It can be prepared as an injection solution using 2% DMSO, 2% Tween 80, 48% PEG300, and 48% water. This data, intended solely for academic reference, demonstrates that Aderbasib at a dosage of 50 mg/kg, administered via intraperitoneal injection to NSG mice following the specified schedule, significantly suppresses the progression of pediatric glioblastoma orthotopic xenografts[1]. |
Synonyms | INCB007839, INCB7839 |
Molecular Weight | 416.47 |
Formula | C21H28N4O5 |
CAS No. | 791828-58-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Aderbasib 791828-58-5 INCB 7839 INCB 007839 INCB-007839 INCB007839 INCB7839 INCB-7839 inhibitor inhibit