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CAS No.: 146535-11-7

Tyrphostin AG1296 Catalog No. CSN12169

Synonyms: AG1296;Tyrphostin;tyrphostin AG1296

AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. It also inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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.
动物研究
剂量
Nud/nud mice: 40 mg/kg, 80 mg/kg^[3] (i.p.), 100 mg/kg^[4] (i.p.) C57Bl/6H and C57Bl/6J (female): 10 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Nud/nud mice: 40 mg/kg, 80 mg/kg^[3] (i.p.), 100 mg/kg^[4] (i.p.) C57Bl/6H and C57Bl/6J (female): 10 mg/kg^[5] (i.p.)
给药途径	i.p.

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
- 3.7552 mL
- 18.7762 mL
- 37.5524 mL
- 5 mM
- 0.7510 mL
- 3.7552 mL
- 7.5105 mL
- 10 mM
- 0.3755 mL
- 1.8776 mL
- 3.7552 mL

技术信息

CAS号

146535-11-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14N2O2

运输

蓝冰

分子量

266.29

别名

AG1296;Tyrphostin;tyrphostin AG1296

溶解度

DMSO	50.0 mg/mL (187.8 mM)
Water	insoluble

动物实验配方

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