Aderbasib |
رقم الكتالوجGC63661 |
Aderbasib (INCB007839) هو مثبط فعّال وفعال عن طريق الفم ومثبط مستهدف منخفض النانو مولار قائم على هيدروكسامات لكل من ADAM10 و ADAM17يُظهر Aderbasib نشاطًا قويًا مضادًا للأورام ويمكن استخدامه لأبحاث السرطان ، بما في ذلك سرطان الغدد الليمفاوية B-cell non-Hodgkin المنتشر ، وسرطان الثدي HER2 ، والأورام الدبقية ، وآخرون
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 791828-58-5
Sample solution is provided at 25 µL, 10mM.
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[1].
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].
[1]. Lois Witters, et al. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9.
[2]. Fei Yuan, et al. ADAM17 is an essential attachment factor for classical swine fever virus. PLoS Pathog. 2021 Mar 8;17(3):e1009393.
Average Rating: 5
(Based on Reviews and 27 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *