AG-490 (Tyrphostin B42)
(Synonyms: 酪氨酸磷酸化抑制剂AG490) 目录号 : GC13854
AG-490 (Tyrphostin B42)是EGFR抑制剂,IC50为0.1 µM, AG-490对JAK2也有抑制作用。
Cas No.:133550-30-8
Sample solution is provided at 25 µL, 10mM.
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]。
| Cell experiment [1]: | |
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Cell lines |
RAW264.7 cell |
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Preparation Method |
Cells were cultured in the presence of RANKL (100 ng/mL) and increasing concentrations of AG-490. |
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Reaction Conditions |
5-50 µM;3days |
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Applications |
AG-490 suppresses RANKL-induced osteoclastogenesis in RAW264.7 cells. |
| Animal experiment [2]: | |
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Animal models |
Female B6C3F1 mice(HM-1 cancer model) |
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Preparation Method |
Mice were daily treated with an intraperitoneal injection of AG-490 (500µg /mouse) or PBS alone as the control. |
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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. |
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| Cas No. | 133550-30-8 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | Soluble in DMSO > 10 mM | 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。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3979 mL | 16.9895 mL | 33.9789 mL |
| 5 mM | 0.6796 mL | 3.3979 mL | 6.7958 mL |
| 10 mM | 0.3398 mL | 1.6989 mL | 3.3979 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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