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Erdafitinib

SKU: orb1303841

描述

Erdafitinib (JNJ-42756493) is a potent, pan-FGFR inhibitor targeting FGFR1-4 with low nanomolar IC50 values. It demonstrates pro-apoptotic and antitumor effects, supporting its research use in oncology for both in vitro cellular studies and in vivo xenograft models of FGFR-altered cancers.

研究领域

Cardiovascular Research, Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

图片与验证

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关键属性

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CAS 号1346242-81-6
MW446.54
纯度99.36% (May vary between batches)
分子式C25H30N6O2
SMILESCOc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(nc2c1)-c1cnn(C)c1
靶点FGFR,Apoptosis
溶解性10% DMSO+40% PEG300+5% Tween 80+45% Saline:8.2 mg/mL (18.36 mM);Ethanol:15 mg/mL (33.59 mM);DMSO:32 mg/mL (71.66 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

生物活性

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靶点 IC50
FGFR2:2.5nM|FGFR4:5.7 nM|FGFR3:3.0nM|FGFR1:1.2 nM
体内
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.
体外
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.
细胞研究
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 trypan blue dye exclusion for the suspension cells, NCI-H716. (Only for Reference)

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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Apoptosis, Inhibitor, FGFR4, FGFR, FGFR1, FGFR2, FGFR3, Fibroblast growth factor receptor, Erdafitinib, JNJ 42756493, JNJ42756493, JNJ-42756493, inhibit

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  • Erdafitinib [orb1226492]

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质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

5 mg
¥ 1,040.00
1 ml x 10 mM (in DMSO)
¥ 1,170.00
10 mg
¥ 1,430.00
25 mg
¥ 1,820.00
50 mg
¥ 2,600.00
100 mg
¥ 3,640.00
500 mg
¥ 8,190.00
发货Usually dispatched within 5-10 working days
批量询价