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抑制剂/激活剂

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凋亡与自噬

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Erdafitinib 厄达替尼; JNJ-42756493

Erdafitinib (JNJ-42756493)是有效的有口服活性的 FGFR 家族抑制剂；抑制FGFR1-4活性的 IC50 分别为1.2, 2.5, 3.0和5.7 nM。

货号：
TK0556
规格：

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	1346242-81-6
生物活性	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.
分子式	C25H30N6O2
分子量	446.54
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 62.5 mg/mL (139.97 mM; Need ultrasonic)
体内研究	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.
体外研究	Erdafitinib (JNJ-42756493) 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. Erdafitinib 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. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively.
文献	•Cancer Discov. 2019 Dec;9(12):1686-1695. •Chem Res Toxicol. 2021 Jun 30. •Oncotarget. 2020 Nov 3;11(44):3921-3932.
纯度及产品资料	98%

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