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AG-82 Sale

(Synonyms: 酪氨酸磷酸化抑制剂25,NSC 676484,RG-50875,Tyrphostin 25,Tyrphostin AG-82) 目录号 : GC11845

An inhibitor of EGF receptor kinase

AG-82 Chemical Structure

Cas No.:118409-58-8

规格 价格 库存 购买数量
5mg
¥381.00
现货
10mg
¥698.00
现货
25mg
¥1,634.00
现货
50mg
¥2,903.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

AG-82 is a cell-permeable, reversible, and competitive inhibitor of tyrosine kinase and epidermal growth factor (EGF) receptor.

Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis [2]. The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival [3].

In the human epidermoid carcinoma cell line A431, AG-82 inhibited the activity of epidermal growth factor receptor kinase with an IC50 value of 3 μM [1]. AG-82 inhibited the GTPase activity of transducin with an IC50 of 7 μM. AG-82 inhibited neuromedin B-induced phosphorylation of p125FAK (focal adhesion kinase). AG-82 blocked the induction of inducible nitric oxide synthase in glial cells and Induced apoptosis in human leukemic cell lines.

References:
[1] Gazit A, Yaish P, Gilon C, et al.  Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors[J]. Journal of medicinal chemistry, 1989, 32(10): 2344-2352.
[2] Levitzki A, Gazit A.  Tyrosine kinase inhibition: an approach to drug development[J]. Science, 1995, 267(5205): 1782.
[3] Herbst R S.  Review of epidermal growth factor receptor biology[J]. International Journal of Radiation Oncology Biology Physics, 2004, 59(2): S21-S26.

化学性质

Cas No. 118409-58-8 SDF
别名 酪氨酸磷酸化抑制剂25,NSC 676484,RG-50875,Tyrphostin 25,Tyrphostin AG-82
化学名 2-[(3,4,5-trihydroxyphenyl)methylene]-propanedinitrile
Canonical SMILES OC1=CC(/C=C(C#N)/C#N)=CC(O)=C1O
分子式 C10H6N2O3 分子量 202.2
溶解度 ≤20mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
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 4.9456 mL 24.728 mL 49.456 mL
5 mM 0.9891 mL 4.9456 mL 9.8912 mL
10 mM 0.4946 mL 2.4728 mL 4.9456 mL
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