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Erdafitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Erdafitinib图片
CAS NO:1346242-81-6
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍

化学性质

StorageStore at -20°C
M.Wt446.54
Cas No.1346242-81-6
FormulaC25H30N6O2
SynonymsJNJ-42756493
Solubilityinsoluble in H2O; ≥15 mg/mL in EtOH; ≥54.5 mg/mL in DMSO
Chemical NameN1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine
Canonical SMILESCN(N=C1)C=C1C2=NC3=CC(N(CCNC(C)C)C4=CC(OC)=CC(OC)=C4)=CC=C3N=C2
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

资料参考

Erdafitinib is an effective, selective and oral bioactive pan-fibroblast growth factor receptor FGFR inhibitor with potential anti-tumor activity and inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.In vitro, Erdafitinib-treated cells reduced proliferation, increased apoptotic death, and reduced cell survival. In vivo experiments, Erdafitinib treatment delayed the growth of NCI-H716 tumors, and when drug treatment was withdrawn, tumor volume increased

试验操作

Cell experiment:[1]

Cell lines

Various colorectal cancer (CRC) cell lines with FGFR wild type (Caco2 and HCA7) and FGFR2 amplification (HCT116, NCI-H716)

Reaction Conditions

72 h incubation

Applications

Erdafitinib significantly decreased cell growth and survival of NCI-H716 cells at concentrations of ≧ 0.5nM, whereas ≧ 5000 nM was required for all other cell lines, including Caco2.

Animal experiment:[1]

Animal models

NMRI nu/nu female mice xenografted with NCI-H716 cellse

Dosage form

40 mg/kg

Administered in the morning three times a week for three weeks by gavage

Applications

In vivo, growth of NCI-H716 tumors was delayed by 5 days by drug treatment alone, although when drug delivery was stopped the relative tumor volume increased compared to control.

Note

The technical data provided above is for reference only.

References:

1. Verstraete M, Debucquoy A, Gonnissen A, et al. In vitro and in vivo evaluation of the radiosensitizing effect of a selective FGFR inhibitor (JNJ-42756493) for rectal cancer. BMC Cancer, 2015, 15: 946.