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Aderbasib Sale

(Synonyms: (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) 目录号 : GC63661

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。

Aderbasib Chemical Structure

Cas No.:791828-58-5

规格 价格 库存 购买数量
5 mg
¥3,600.00
现货
10 mg
¥5,850.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

Cas No. 791828-58-5 SDF
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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4011 mL 12.0057 mL 24.0113 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 mL
10 mM 0.2401 mL 1.2006 mL 2.4011 mL
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