Dovitinib (TKI258) Lactate
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.
Dovitinib (TKI258) Lactate对FGFR1–3的IC50值约为10 nmol/L.
在约10%的乳腺癌中,观察到成纤维细胞生长因子受体1(FGFR1)与FGFR2扩增,此现象与乳腺癌不良预后相关.Dovitinib(TKI258)是一种口服的酪氨酸激酶抑制剂(TKI),作用于FGFR1-3\VEGFR1-3和血小板衍生生长因子受体(PDGFR).
体外:在FGFR1与FGFR2扩增的细胞系中,Dovitinib呈剂量依赖性地降低pFRS2和pERK/MAPK的浓度.在MDA-MB-134细胞与SUM52细胞中,Dovitinib对细胞生长抑制的IC50值分别为190 nmol/L和180 nmol/L.相反地,在无FGFR1和FGFR2扩增的11种乳腺癌细胞系中,Dovitinib的IC50值均大于2,000 nmol/L[1].
体内:在体内模型(携带8个FGFR1基因拷贝的HBCx-2乳腺癌原代细胞异种移植模型)中,30 mg/kg Dovitinib抑制肿瘤生长,50 mg/kg Dovitinib使肿瘤消退.此外,在HBCx-3细胞异种移植模型中,给予40 mg/kg Dovitinib,每天1次,持续35天,可以使肿瘤消退[1].
临床试验:共81例患者入组.在5例FGFR1扩增/HR阳性乳腺癌患者与1例FGFR1非扩增/HR阳性乳腺癌患者中,观察到持续6个月以上的未确定反应或病情稳定.使用qPCR鉴定FGFR1\FGFR2或FGF3扩增,基于不同的FGF扩增,对HR阳性乳腺癌患者进行分组.相对于非FGF途径扩增的乳腺癌患者(目标病灶增加了12.0%),FGF途径扩增的乳腺癌患者目标病灶平均减少了21.1%[1].
参考文献:
[1] André F, Bachelot T, Campone M, Dalenc F, Perez-Garcia JM, Hurvitz SA, Turner N, Rugo H, Smith JW, Deudon S, Shi M, Zhang Y, Kay A, Porta DG, Yovine A, Baselga J. Targeting FGFR with dovitinib (TKI258): preclinical and clinical data in breast cancer. Clin Cancer Res. 2013 Jul 1;19(13):3693-702.
Storage | Store at -20°C |
M.Wt | 500.52 |
Cas No. | 915769-50-5 |
Formula | C24H29FN6O5 |
Solubility | insoluble in EtOH; ≥10.62 mg/mL in DMSO; ≥168.2 mg/mL in H2O |
Chemical Name | 4-amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate hydra |
SDF | Download SDF |
Canonical SMILES | FC1=C(C(N)=C(C2=O)C3=NC4=C(N3)C=C(N5CCN(C)CC5)C=C4)C(N2)=CC=C1.CC(O)C(O)=O.O |
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
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