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- PKD (Protein kinase D)
- Aderbasib
Aderbasib
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。
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包装价格促销价数量
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5mg￥4312.003450.00- +
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10mg￥7012.005610.00- +
- 货号: ajcx36112
- CAS: 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
- 纯度: ＞98%
- 溶解度: DMSO : 100 mg/mL (240.11 mM; Need ultrasonic)
- 储存: Store at -20°C
- 库存: 现货
Background
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.
