产品属性：
产品名称 | 规格 | CAS号 | 型号 |
Erdafitinib | 5mg 10mg 50mg 100mg | 1346242-81-6 | EY-Y0165357 |
Cas No.1346242-81-6
别名 N/A
化学名 N/A
分子式 C25H30N6O2
分子量 446.54
溶解度 DMSO : ≥ 33 mg/mL (73.90 mM)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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.
Erdafitinib inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8 nM. JNJ-42756493 binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd value for VEGFR2 is higher at 6.6 nM. JNJ-42756493 inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively[1].
In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors[1].
References:
[1]. Perera TP, et al. Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Mol Cancer Ther. 2017 Mar 24. pii: molcanther.0589.2016.
关键字： 1346242-81-6;C25H30N6O2;Erdafitinib;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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