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CAS No.: 133550-35-3

AG 494 Catalog No. CSN21119

Synonyms: Tyrphostin AG 494

AG-494 is an inhibitor of EGFR with an IC50 value of 0.7 µM and it is inactive toward ErbB2, PDGFR and insulin receptor kinase.

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技术信息

生物活性

描述Many of the tyrosine kinase enzymes which are early components of the growth signal transduction pathway in mammalian cells are encoded by proto-oncogenes, and their transformation or overexpression has been shown to occur in a large percentage of clinical cancers. The epidermal growth factor receptor (EGFR), one of the tyrosine kinase enzymes, has thus become important target for cancer therapy ^[1]. AG-494 is capable of selectively inhibiting the EGFR tyrosine kinase activity in vitro as compared to a variety of tyrosine kinases, including the closely related HER-2/Neu receptor in the cell-free kinase assay. AG-494 inhibits autophosphorylation of EGFR with IC₅₀ value of 1.1 ± 0.24 μM. AG-494 inhibits 50% of TPA (phorbol ester)- and LPA (lysophosphatidic acid)-dependent [³H]thymidine uptake at ~5 μM, whereas EGF-dependent [³H]thymidine uptake is inhibited at ~10.5 μM. These results imply that AG-494 exerts its antimitogenic effect by inhibiting a signal transduction element downstream of the EGFR ^[2]. EGF potentiates BMP9-induced early and late osteogenic markers of mesenchymal stem cells (MSCs), which can be effectively inhibited by AG-494 ^[3].
参考文献

[1] Bridges AJ. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76. doi: 10.1021/jm9503613.
[2] Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997 Jun 30;410(2-3):187-90. doi: 10.1016/s0014-5793(97)00580-2.
[3] Liu X. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med. 2013 Sep;17(9):1160-72. doi: 10.1111/jcmm.12097. Epub 2013 Jul 11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5679 mL
- 17.8394 mL
- 35.6788 mL
- 5 mM
- 0.7136 mL
- 3.5679 mL
- 7.1358 mL
- 10 mM
- 0.3568 mL
- 1.7839 mL
- 3.5679 mL

技术信息

CAS号

133550-35-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H12N2O3

运输

蓝冰

分子量

280.28

别名

Tyrphostin AG 494

溶解度

DMSO	50.0 mg/mL (178.4 mM)

动物实验配方

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AG 494 Catalog No. CSN21119

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