CAS NO: | 1346242-81-6 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
Storage | Store at -20°C |
M.Wt | 446.54 |
Cas No. | 1346242-81-6 |
Formula | C25H30N6O2 |
Synonyms | JNJ-42756493 |
Solubility | insoluble in H2O; ≥15 mg/mL in EtOH; ≥54.5 mg/mL in DMSO |
Chemical Name | N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine |
Canonical SMILES | CN(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。 |
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 In vivo experiments, Erdafitinib treatment delayed the growth of NCI-H716 tumors, and when drug treatment was withdrawn, tumor volume increased
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. |