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Tyrphostin AG1296

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Chemical Structure| 146535-11-7 同义名 : AG 1296
CAS号 : 146535-11-7
货号 : A104725
分子式 : C16H14N2O2
纯度 : 99%+
分子量 : 266.295
MDL号 : MFCD00270913
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(131.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PDGFR

    PDGFR, IC50:0.3 μM-0.5 μM

  • FGFR

    FGFR (Swiss 3T3), IC50:12.3 μM

  • c-Kit

    c-Kit (Swiss 3T3), IC50:1.8 μM
描述 Platelet-derived growth factors (PDGFs) are composed of five kinds of ligand dimers, PDGF-AA, -BB, -AB, -CC, and -DD, which bind to three kinds of their receptor dimmers, PDGF receptor (PDGFR) αα, αβ, and ββ, with different affinities. PDGF and its receptors participate in various physiological processes such as embryonal development and wound healing. AG1296 potently inhibits human PDGF α- and β-receptors with IC50 of 0.3 - 0.5 μM, as well as the related stem cell factor receptor (c-Kit), but has no effect on EGFR[3]. The combination treatment of MK-2206 (5 μM) and tyrphostin AG 1296 (4 μM) for 48h induced more pronounced cell apoptosis than either MK-2206 or tyrphostin AG 1296 alone, and additive inhibition of cell migration and invasion in anaplastic thyroid carcinoma cells[4]. Consistently, intraperitoneal administration of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) induced more significant inhibition characteristics on growth of KAT4 cells in nud/nud mice than either MK-2206 or tyrphostin AG 1296 alone[4]. Intraperitoneal injection of AG1296 (2 mg/kg, every other day) for 3 weeks decreased atherosclerotic plaques area in carotid arteries in ApoE-/- mice by 41.5% and inhibited inflammatory responses (49.0% and 51.8% lower in IL-6 and TNF-a, respectively)[5].
作用机制 AG1296 inhibits human PDGF α- and β-receptors by inhibiting phosphorylation of individual autophosphorylation sites of the PDGF receptor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.76mL

0.75mL

0.38mL

18.78mL

3.76mL

1.88mL

37.55mL

7.51mL

3.76mL
参考文献

[1]Kovalenko M, Ronnstrand L, et al. Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Biochemistry. 1997 May 27;36(21):6260-9.

[2]Kovalenko M, Gazit A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1;54(23):6106-14.

[3]Kovalenko M, Gazit A, Böhmer A, Rorsman C, Rönnstrand L, Heldin CH, Waltenberger J, Böhmer FD, Levitzki A. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1;54(23):6106-14. PMID: 7954456.

[4]Che HY, Guo HY, Si XW, You QY, Lou WY. Additive effect by combination of Akt inhibitor, MK-2206, and PDGFR inhibitor, tyrphostin AG 1296, in suppressing anaplastic thyroid carcinoma cell viability and motility. Onco Targets Ther. 2014 Mar 14;7:425-32. doi: 10.2147/OTT.S57324. PMID: 24665203; PMCID: PMC3961587.

[5]Dong M, Zhou C, Ji L, Pan B, Zheng L. AG1296 enhances plaque stability via inhibiting inflammatory responses and decreasing MMP-2 and MMP-9 expression in ApoE-/- mice. Biochem Biophys Res Commun. 2017 Aug 5;489(4):426-431. doi: 10.1016/j.bbrc.2017.05.159. Epub 2017 May 27. PMID: 28559142.