Altiratinib
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.
Altiratinib (DCC-2701)是c-MET/TIE-2/VEGFR的有效抑制剂,IC50值分别为2.7\8.0和9.2 nM[1].
肝细胞生长因子受体(c-MET)是肝细胞生长因子的酪氨酸激酶受体,对伤口愈合和胚胎发育是必不可少的.TEK酪氨酸激酶(TIE-2)是血管生成素-1(ANG-1)的受体,对内皮细胞-平滑肌细胞的通讯至关重要.VEGFR是血管内皮生长因子的酪氨酸激酶受体,参与血管生成和血管发生.
Altiratinib (DCC-2701)是一种强效的c-MET/TIE-2/VEGFR抑制剂.Alectinib有效抑制MET激酶,激活癌基因MET突变,也抑制TRKA\TRKB和TRKC激酶,IC50值分别为0.85\4.6和0.83 nM.在过表达MET的EBC-1非小细胞肺癌和MKN-45胃癌细胞系中,altiratinib抑制MET的磷酸化,IC50值分别为0.85和2.2 nM.在VEGF刺激的HUVECs中,altiratinib抑制 VEGFR2磷酸化,IC50值为4.7 nM.在HUVECs和EA.hy926细胞中,altiratinib抑制ANG-1刺激的TIE2磷酸化,IC50值分别为1.0和2.6 nM[1].
在MET扩增的MKN-45异种移植模型中,24小时内30 mg/kg剂量的altiratinib抑制大于95％的MET磷酸化[1].在SKOV3细胞异种移植裸鼠中,10或20 mg/kg的DCC-2701治疗28天显著减少53％和52％的肿瘤负荷[2].
参考文献：
[1]. Smith BD, Kaufman MD, Leary CB, et al. Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2. Mol Cancer Ther, 2015.
[2]. Kwon Y, Smith BD, Zhou Y, et al. Effective inhibition of c-MET-mediated signaling, growth and migration of ovarian cancer cells is influenced by the ovarian tissue microenvironment. Oncogene, 2015, 34(2): 144-153.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 510.46 |
| Cas No. | 1345847-93-9 |
| Formula | C26H21F3N4O4 |
| Solubility | ≥21.55 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | N-(4-((2-(cyclopropanecarboxamido)pyridin-4-yl)oxy)-2,5-difluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=C(NC(C2(C(NC3=C(F)C=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C(F)=C3)=O)CC2)=O)C=C1 |
| 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
相关生物数据
