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Aderbasib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aderbasib图片
CAS NO:791828-58-5
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Aderbasb (INCB007839) 是一种有效的、具有口服活性的、靶向特异性的低纳摩尔 ADAM10 和 ADAM17 抑制剂。Aderbasb 表现出强大的抗肿瘤活性,可用于癌症研究,包括弥漫性大 B 细胞非霍奇金淋巴瘤,HER2+ 乳腺癌,胶质瘤等。
Cas No.791828-58-5
别名(6S,7S)-7-[(羟基氨基)甲酰基]-6-[(4-苯基-1-哌嗪基)甲酰基]-5-氮杂螺[2.5]辛烷-5-甲酸甲酯,INCB007839; INCB7839
分子式C21H28N4O5
分子量416.47
溶解度DMSO : 100 mg/mL (240.11 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.