CAS: 118409-58-8; 2-(3,4,5-Trihydroxybenzylidene)Malononitrile
该化合物是上皮生长因子受体(EGFR)强力抗体的选择性和强力抑制剂,作为Trrphostin家族的成员,它与EGFR的APTP约束性网站有竞争关系,有效地阻断了它的自对光和下游信号路径.该复合体在其他相关的亲属关系中具有高度的特性,使它成为研究EGFR调解的细胞过程的宝贵工具.Typhostin 25在调查EGFR在细胞扩散,分化和组合中作用的研究中被广泛使用.其精细的行动机制和一致的抑制性活动有助于其在体外和体内研究中的可靠性.该复合体对于解释依赖EGFR信号的级联的分子基础特别有用.
- 英文名称2-(3,4,5-Trihydroxybenzylidene)Malononitrile
- 中文名称酪氨酸磷酸化抑制剂25
- IUPAC名称2-(3,4,5-trihydroxybenzylidene)malononitrile
- 其它别名[3,4,5-Trihydroxybenzylidene]Malononitrile; Ag 82; Alpha-Cyano-(3,4,5-Trihydroxy)Cinnamonitrile; Tyrphostin 25; Tyrphostin Ag 82
- CAS编号118409-58-8
- MFCD编号:MFCD00133900
- FDA UNII编号:C878BF87UY
- 分子式:C10H6N2O3分子量:202.17
- 产品CID: 235462
- 产品分类生物化工 → 氨基酸及其衍生物 → 酪氨酸类衍生物
物理性质
- 熔点-220 °C dec.
- 沸点500.8±50.0 °C at 760 mmHg
- 闪点256.7±30.1 °C
- 密度1.6±0.1 g/cm3
- pKa:7.10±0.23(预测)
- PSA:108.27
- LogP:0.55
- 折射率1.743
- 蒸汽压0.0±1.3 mmHg at 25°C
- 溶解性DMSO: >50 mg/mL, Clear, Yellow To Orange
- 敏感性如果遵照规格使用和储存则不会分解，未有已知危险反应
- 外观形态黄绿色深黄色固体
- 储存条件2-8°C
- 产品应用该化合物是上皮生长因子受体(EGFR)强力抗体激素激素性激素小分子抑制剂,在临床前型模型中表现出抗脉冲活动.在体外,AG-82 有效封隔EG FR 自动光电阻,导致抑制对细胞扩散,生存和分化至关重要的MAPK和PI3K/AKT等下游信号路径.这种抑制导致EGR-50876成为研究EGVR-FR信号,癌症细胞扩散和EG-FFR定向治疗战略的宝贵研究工具.在VIVO,AK-82 减少XENOGRAFT 模型中的肿瘤生长,确认有效路径抑制和翻译相关性.通过瞄准一个关键源驱动器,AAG82 干扰支持肿瘤发展的信号网络.这些特性使得RG-50775成为研究GFFER信号,癌细胞扩散以及EG-FR驱动的定向治疗策略的宝贵研究手段.
MSDS等安全信息
上下游产品
CAS号13677-79-7 五倍子醛 | CAS号109-77-3 丙二腈合成工艺路线路线简述
📜丙二腈,Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于水体系中,化学反应生成酪氨酸磷酸化抑制剂25
参考文献:Rosenmund; Boehm,Justus Liebigs Annalen Der Chemie,1924,Vol. 437,P. 143
标题:Rosenmund; Boehm,Justus Liebigs Annalen Der Chemie,1924,Vol. 437,P. 143
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2902300000-甲苯
2902500000-苯乙烯 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:WO-9911652-A1
优先权日:1997-09-02
标 题 :Role of tyrosine phosphorylation of a cellular protein in adeno-associated virus 2-mediated transgene expression
发明人：SRIVASTAVA ARUN; QING KEYUN; WANG XU-SHAN; PONNAZHAGAN SELVARANGAN; BAJPAI ANIL
权利人:ADVANCED RES & TECH INST; SRIVASTAVA ARUN; QING KEYUN; WANG XU SHAN; PONNAZHAGAN SELVARANGAN; BAJPAI ANIL
摘要:The present invention identifies a protein, designated the D-sequence-binding protein (D-BP), is phosphorylated at tyrosine residues and blocks AAV-mediated transgene expression in infected cells by inhibiting the leading strand viral DNA synthesis. More particularly, the present invention demonstrates that D-BP is phosphorylated by EGF-R protein tyrosine kinase. Methods of increasing transcription and promoting replication of transgenes exploiting this information are disclosed therein.
专利号:US-9907753-B2
优先权日:2010-03-19
标 题 :Lipid vesicle compositions and methods of use
发明人：IRVINE DARRELL J; MOON JAEHYUN
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.
专利号:US-7052692-B1
优先权日:1997-09-02
标题:Role of tyrosine phosphorylation of a cellular protein in adeno-associated virus 2-mediated transgene expression
发明人：SRIVASTAVA ARUN; QING KEYUN; WANG XU-SHAN; PONNAZHAGAN SELVARANGAN; BAJPAI ANIL
权利人:ADVANCED RES & TECH INST
摘要:The present invention identifies a protein, designated the D-sequence-binding protein (D-BP), is phosphorylated at tyrosine residues and blocks AAV-mediated transgene expression in infected cells by inhibiting the leading strand viral DNA synthesis. More particularly, the present invention demonstrates that D-BP is phosphorylated by EGF-R protein tyrosine kinase. Methods of increasing transcription and promoting replication of transgenes exploiting this information are disclosed herein.
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1. Gazit, A., Yaish, P., Gilon, C., et al. Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors. J. Med. Chem. 32(10), 2344-2352 (1989).合成参考文献
参考文献:10.1007/bf00177440
摘要:Zenke K, Nakagawa K, Kumon Y, Ohta S, Hatakeyama T, Sakaki S. A strategy for selective anti-cancer drug concentration increase in rat glioma tissue with Ca(2+)-channel blocker co-administration: calcium kinetics in intra-glioma arteriolar smooth muscle cells. J Neurooncol. 1996 Oct;30(1):25–36. doi: 10.1007/bf00177440.
参考文献:10.1016/0006-8993(96)00417-9|10.1016/s0006-8993(96)00417-9
摘要:Kong L, McMillian MK, Maronpot R, Hong J. Protein tyrosine kinase inhibitors suppress the production of nitric oxide in mixed glia, microglia-enriched or astrocyte-enriched cultures. Brain Research. 1996 Aug;729(1):102–9. doi: 10.1016/0006-8993(96)00417-9.
参考文献:10.1080/01616412.1996.11740435
摘要:Marton LS, Weir BKA, Zhang H. Tyrosine phosphorylation and [Ca2+]ielevation induced by hemolysate in bovine endothelial cells: Implications for cerebral vasospasm. Neurological Research. 1996 Aug;18(4):349–53. doi: 10.1080/01616412.1996.11740435.
参考文献:10.1007/s004320050290
摘要:Partik G, Hochegger K, Schörkhuber M, Marian B. Inhibition of epidermal-growth-factor-receptor-dependent signalling by tyrphostins A25 and AG1478 blocks growth and induces apoptosis in colorectal tumor cells in vitro. Journal of Cancer Research and Clinical Oncology. 1999 Jun 02;125(7):379–88. doi: 10.1007/s004320050290.
参考文献:10.1152/jappl.1999.87.1.363
摘要:Czapla MA, Simakajornboon N, Holt GA, Gozal D. Tyrosine kinase inhibitors modulate the ventilatory response to hypoxia in the conscious rat. J Appl Physiol (1985). 1999 Jul;87(1):363–9. doi: 10.1152/jappl.1999.87.1.363.
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