GlpBio

AG-490 (Tyrphostin B42)

目录号: GC13854纯度: >98.00%同义词: 酪氨酸磷酸化抑制剂AG490
AG-490 (Tyrphostin B42)是EGFR抑制剂,IC50为0.1 µM, AG-490对JAK2也有抑制作用。
AG-490 (Tyrphostin B42)
Cas No.: 133550-30-8
规格价格库存数量操作
10mg¥284.00现货
1
25mg¥494.00现货
1
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产品描述 Description

AG-490 (Tyrphostin B42) is EGFR inhibitor with IC50 of 0.1 µM, AG-490 also has an inhibitory effect on JAK2[1-3].

AG-490(5-50 µM;3days) suppresses RANKL-induced osteoclastogenesis in RAW264.7 cells[4]. AG490(20 µM; 4 h) inhibits hOAT3 transport activity[5]. AG-490(10 µM)suppresses interleukin-34-mediated osteoclastogenesis in mice bone marrow macrophages[6].

AG-490(5-15 µM;i.p;) exerted protection effects by preventing the neural apoptosis in vivo[7]. In tumor mice, AG-490(500 µg/mouse;i.p;11days) treatment significantly inhibited subcutaneous tumor growth[8].

References:
[1]. DuhÉ RJ, Clark EA, et,al. Characterization of the in vitro kinase activity of a partially purified soluble GST/JAK2 fusion protein. Mol Cell Biochem. 2002 Jul;236(1-2):23-35. doi: 10.1023/a:1016186907376. PMID: 12190118.
[2]. Luo C, Laaja P. Inhibitors of JAKs/STATs and the kinases: a possible new cluster of drugs. Drug Discov Today. 2004 Mar 15;9(6):268-75. doi: 10.1016/S1359-6446(03)03014-9. PMID: 15003245.
[3]. Gazit A, Osherov N, et,al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991 Jun;34(6):1896-907. doi: 10.1021/jm00110a022. PMID: 1676428.
[4]. Li CH, Zhao JX, et,al. AG490 inhibits NFATc1 expression and STAT3 activation during RANKL induced osteoclastogenesis. Biochem Biophys Res Commun. 2013 Jun 14;435(4):533-9. doi: 10.1016/j.bbrc.2013.04.084. Epub 2013 May 7. PMID: 23665018.
[5]. Zhang J, Liu C, et,al. AG490, a JAK2-specific inhibitor, downregulates the expression and activity of organic anion transporter-3. J Pharmacol Sci. 2018 Mar;136(3):142-148. doi: 10.1016/j.jphs.2018.01.006. Epub 2018 Feb 8. PMID: 29487013; PMCID: PMC7863619.
[6]. Cheng X, Wan QL, et,al. AG490 suppresses interleukin-34-mediated osteoclastogenesis in mice bone marrow macrophages. Cell Biol Int. 2017 Jun;41(6):659-668. doi: 10.1002/cbin.10771. Epub 2017 Apr 19. PMID: 28378938.
[7]. Fan L, Zhou L. AG490 protects cerebral ischemia/reperfusion injury via inhibiting the JAK2/3 signaling pathway. Brain Behav. 2021 Jan;11(1):e01911. doi: 10.1002/brb3.1911. Epub 2020 Oct 23. PMID: 33098244; PMCID: PMC7821583.
[8]. Kobayashi A, Tanizaki Y, et,al. AG490, a Jak2 inhibitor, suppressed the progression of murine ovarian cancer. Eur J Pharmacol. 2015 Nov 5;766:63-75. doi: 10.1016/j.ejphar.2015.09.039. Epub 2015 Sep 26. PMID: 26410360.

AG-490 (Tyrphostin B42)是EGFR抑制剂,IC50为0.1 µM, AG-490对JAK2也有抑制作用[1-3]。

AG-490 (5-50 µM;3days)抑制RANKL诱导的RAW264.7细胞破骨生成[4]。AG-490(20µM;4 h)抑制hOAT3转运活性[5]。AG-490(10µM)抑制白细胞介素-34介导的小鼠骨髓巨噬细胞破骨生成[6]。

AG-490(5-15 µM;i.p)在体内通过阻止神经细胞凋亡发挥保护作用[7]。在肿瘤小鼠中,AG-490 (500 µg/mouse;i.p;11days)治疗可显著抑制皮下肿瘤生长[8]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

RAW264.7 cell

Preparation Method

Cells were cultured in the presence of RANKL (100 ng/mL) and increasing concentrations of AG-490.

Reaction Conditions

5-50 µM;3days

Applications

AG-490 suppresses RANKL-induced osteoclastogenesis in RAW264.7 cells.
Animal experiment [2]:

Animal models

Female B6C3F1 mice(HM-1 cancer model)

Preparation Method

Mice were daily treated with an intraperitoneal injection of AG-490 (500µg /mouse) or PBS alone as the control.

Dosage form

500 µg/mouse; i.p;11days

Applications

AG-490 treatment significantly suppressed subcutaneous tumor growth compared with control.

References:

[1]. Li CH, Zhao JX, et,al. AG490 inhibits NFATc1 expression and STAT3 activation during RANKL induced osteoclastogenesis. Biochem Biophys Res Commun. 2013 Jun 14;435(4):533-9. doi: 10.1016/j.bbrc.2013.04.084. Epub 2013 May 7. PMID: 23665018.
[2]. Kobayashi A, Tanizaki Y, et,al. AG490, a Jak2 inhibitor, suppressed the progression of murine ovarian cancer. Eur J Pharmacol. 2015 Nov 5;766:63-75. doi: 10.1016/j.ejphar.2015.09.039. Epub 2015 Sep 26. PMID: 26410360.

产品文档 Product Documents

Purity:>98.00%

相关生物学数据Related Biological Data

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化学性质Chemical Properties

CAS 号
133550-30-8
同义词
酪氨酸磷酸化抑制剂AG490
化学名
(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
SMILES
C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N
分子式
C17H14N2O3
分子量
294.3 g/mol
溶解性
≥60mg/mL in DMSO
保存条件
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°C，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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol