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AG-1024 Sale

(Synonyms: Tyrphostin AG 1024) 目录号 : GC13697

A selective inhibitor of IGF-1R

AG-1024 Chemical Structure

Cas No.:65678-07-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥462.00
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5mg
¥420.00
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10mg
¥630.00
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50mg
¥1,575.00
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100mg
¥2,520.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment: [1]

Cell lines

MCF-7

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 nM, 5 days for cell proliferation inhibition 10 nM, 48 hours for apoptosis induction

Applications

The Tyrphostin AG-1024 induced a marked decrease of cell proliferation in a time-dependent manner. It also potently induced cell apoptosis with a 20.1 % of apoptotic cells.

Animal experiment : [2]

Animal models

Female nude mice implanted with Ba/F3-p210 cells

Dosage form

Intraperitoneal injection, 30 μg in100 μl, once per day for 10 days

Applications

After injection with Ba/F3-p210 cells (Bcr-Abl expressing cells), nude mice were injected after 6 days with PBS 0.1 ml (control) or Tyrphostin AG1024 30 μg/100 μl (1 μl of 980 μM). The growth of the Ba/F3-p210 xenografts was significantly delayed when mice were treated with Tyrphostin AG1024.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wen B, Deutsch E, Marangoni E, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. British journal of cancer, 2001, 85(12): 2017.

[2] Deutsch E, Maggiorella L, Wen B, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. British journal of cancer, 2004, 91(9): 1735-1741.

产品描述

AG1024 is an inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) that specifically inhibits autophosphorylation of IGF-1R and IR with IC50 values of 7μM and 57 μm, respectively [1].

AG1024 has shown to inhibit IGF-1- and insulin-stimulated cellular proliferation in NIH-3T3 mouse fibroblast cells with IC50 values of 0.4μM and 0.1μM, respectively. Additionally, AG1024 shows to block tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18μM and 80μM [1].

AG1024 has been reported to block receptor tyrosine kinase activity, resulting in abolishment of MAPK and Akt pathways and inhibition of cell growth. Moreover, studies showed that AG1024 concentration-dependently inhibited E2 stimulation in MCF-7:PF cells [2].

References:
[1] Párrizas M1, Gazit A, Levitzki A, Wertheimer E, LeRoith D. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.
[2] Fan P1, Agboke FA1, McDaniel RE1, Sweeney EE1, Zou X1, Creswell K1, Jordan VC2.Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer. 2014 Jan; 50(2):457-68.

Chemical Properties

Cas No. 65678-07-1 SDF
别名 Tyrphostin AG 1024
化学名 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile
Canonical SMILES CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O
分子式 C14H13BrN2O 分子量 305.17
溶解度 ≥ 15.25mg/mL in DMSO 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 3.2769 mL 16.3843 mL 32.7686 mL
5 mM 0.6554 mL 3.2769 mL 6.5537 mL
10 mM 0.3277 mL 1.6384 mL 3.2769 mL
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