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- 2026年07月07日
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- CAS号：
1612888-66-0
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥266.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥542.0 |
| 规格： | 5mg | 产品价格： | ￥596.0 |
| 规格： | 10mg | 产品价格： | ￥856.0 |
| 规格： | 25mg | 产品价格： | ￥1720.0 |
| 规格： | 50mg | 产品价格： | ￥2584.0 |
| 规格： | 100mg | 产品价格： | ￥3720.0 |
| 规格： | 200mg | 产品价格： | ￥5184.0 |
Product Introduction
Bioactivity
| 名称 | Alofanib |
| 描述 | Alofanib (RPT835) is a selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect on FGF2-induced phosphorylation of FRS2a in KATO III cells (IC50 <10 nM). It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding. |
| 细胞实验 | SKOV3 cells were treated with alofanib (10, 100, and 1000 μM) for 72 h and whole-cell lysates were immunoblotted. |
| 体外活性 | In SKOV3 cell line, Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2. It has a low cytotoxic effect on ovarian cancer cells [1]. Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumor types (triple-negative breast cancer, melanoma, and ovarian cancer), alofanib inhibits FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose-dependently inhibits the proliferation and migration of human and mouse endothelial cells (GI50: 11-58 nmol/l) compared with brivanib and bevacizumab [2]. |
| 体内活性 | Alofanib (i.v.) significantly in a dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. Alofanib suppresses angiogenesis in the ovarian cancer mouse model[1]. In an FGFR-driven human tumor xenograft model, oral administration of alofanib is well tolerated and results in potent antitumor activity[2]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.84 mM), Sonication is recommended. H2O : Insoluble DMSO : 55 mg/mL (133.04 mM), Sonication is recommended. |
| 关键字 | RPT-835 | RPT 835 | Inhibitor | inhibit | Fibroblast growth factor receptor | FGFR2 | FGFR | Apoptosis | Alofanib |
| 相关产品 | Formamide | Urea | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Ferulic Acid | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | NO PAINS Compound Library | Preclinical Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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