Tyrphostin AG 1296

    
98%

Tyrphostin AG 1296

源叶(MedMol)
S88036 一键复制产品信息
146535-11-7
C16H14N2O2
266.29
6,7-二甲氧基-2-苯基喹喔啉;AG 1296;6,7-Dimethoxy-2-Phenylquinoxaline;6,7-Dimethoxy-3-Phenylquinoxaline
货号 规格 价格 上海 北京 武汉 南京 购买数量
S88036-2mg 98% ¥80.00 2 - - -
S88036-5mg 98% ¥132.00 6 - - -
S88036-10mg 98% ¥200.00 6 - - -
S88036-25mg 98% ¥360.00 6 - - -
S88036-50mg 98% ¥680.00 货期:2-3天 - - -
S88036-100mg 98% ¥1100.00 货期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range

产品描述: Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range
靶点: PDGFRα;PDGFRβ;Apoptosis; FGFR; FLT; PDGFR; c-Kit
体内研究: Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo. Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype. Animal Model: Nud/nud mice are injected with A375R cells Dosage: 40, 80 mg/kg Administration: I.p. daily for two weeks Result: Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
参考文献: 1. Gazit A, etm, al. Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. Comparative Study J Med Chem. 1996 May 24; 39(11): 2170-7 2. Kovalenko M, et, al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1; 54(23): 6106-14. 3. Tse KF, et, al. Inhibition of the transforming activity of FLT3 internal tandem duplication mutants from AML patients by a tyrosine kinase inhibitor. Leukemia. 2002 Oct; 16(10): 2027-36. 4. Li Y, et, al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells. Onco Targets Ther. 2015 May 14; 8: 1043-51. 5. Dong M, et, al. 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.
溶解性: Soluble  in  DMSO
保存条件: 2-8℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.755 ml 18.777 ml 37.553 ml
5 mM 0.751 ml 3.755 ml 7.511 ml
10 mM 0.376 ml 1.878 ml 3.755 ml
50 mM 0.075 ml 0.376 ml 0.751 ml
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