产品信息
抗原名称
FGFR
商品描述
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.
分子量
446.54
纯度
98%
可溶性
DMSO : 62.5 mg/mL (139.97 mM; Need ultrasonic)
外观
Yellow Solid
In vitro(体外研究)
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.
In vivo(体内研究)
In 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.
背景
别名
厄达替尼
分子式
C25H30N6O2
CAS号
1346242-81-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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