Fruquintinib(HMPL-013)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:对VEGFR1\2和3的IC50分别为33 nmol/L\35 nmol/L和 0.5 nmol/L
VEGF/VEGFR信号是新型癌症疗法发展的重要靶标.VEGF抑制剂的一个挑战是在可耐受的剂量下实现持续靶点抑制,以前发现其在耐受剂量下只具有长效生物学效应.Fruquintinib是VEGFR1\2和3酪氨酸激酶的强效高选择性小分子抑制剂,用于癌症治疗.
体外实验:Fruquintinib抑制VEGFR2,IC50为25 nmol/L.对253种激酶评估了fruquintinib的激酶选择性.结果表明,fruquintinib抑制VEGFR家族成员,对RET\FGFR-1和c-kit激酶的抑制作用较弱[1].
在体实验:在多种肿瘤异种移植模型中评估了fruquintinib的抗肿瘤活性.胃癌BGC-823模型的结果表明,实现大于80％的肿瘤生长抑制至少需要药物浓度保持EC85以上约8小时.BGC-823对fruquintinib最敏感[1].
临床试验:Fruquintinib (HMPL-013)目前处于II期临床研究.I期药代动力学数据分析显示,最大耐受剂量的fruquintinib每日一次口服给药,可以完全抑制VEGFR2,每天抑制作用达24 小时[1].
参考文献：
[1] Sun Q, Zhou J, Zhang Z, Guo M, Liang J, Zhou F, Long J, Zhang W, Yin F, Cai H, Yang H, Zhang W, Gu Y, Ni L, Sai Y, Cui Y, Zhang M, Hong M, Sun J, Yang Z, Qing W, Su W, Ren Y. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 393.39 |
| Cas No. | 1194506-26-7 |
| Formula | C21H19N3O5 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥6.35 mg/mL in DMSO |
| Chemical Name | (Z)-6-((6,7-dimethoxyquinazolin-4-yl)oxy)-N,2-dimethylbenzofuran-3-carbimidic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(O1)=C(/C(O)=N/C)C2=C1C=C(OC3=NC=NC4=CC(OC)=C(OC)C=C43)C=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
