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JNJ-42756493(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。
JNJ-42756493(Erdafitinib)图片
CAS NO:1346242-81-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)446.54
FormulaC25H30N6O2
CAS No.1346242-81-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 89 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 89 mg/mL (199.3 mM)
Other infoChemical Name: N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine
InChi Key: OLAHOMJCDNXHFI-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
SMILES Code: CC(NCCN(C1=CC(OC)=CC(OC)=C1)C2=CC=C3N=CC(C4=CN(C)N=C4)=NC3=C2)C
SynonymsJNJ 42756493; JNJ-42756493; JNJ42756493
实验参考方法
In Vitro

In vitro activity: JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival.


Kinase Assay: Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.


Cell Assay: The effect of varying drug concentrations on cell growth and survival is evaluated at 72 h using sulforhodamine B (SRB) assay for the adherent cells (HCT116, HCA7, Caco2 and NCI-H716 cells ) and trypan blue dye exclusion for the suspension cells, NCI-H716.

In VivoIn vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components.
Animal modelNMRI nu/nu female mice
Formulation & DosageFormulated in cyclodextrin; 40 mg/kg
ReferencesBMC Cancer. 2015 Dec 16;15:946; Cancer Res. 2014, 74(19 Suppl): Abstract.