EGFR-IN-8|2407957-87-1|-陌孚医药/Medlife

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EGFR-IN-8

目录号: PL02815 纯度: ≥98%

CAS No. :2407957-87-1

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中文名称	EGFR-IN-8
英文名称	EGFR-IN-8
英文别名	EGFR-IN-8;N-(3-Chloro-4-(5-(3-(3-(4-(cyclopropanecarboxamido)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1,2,4-oxadiazol-3-yl)phenyl)nicotinamide
Cas No.	2407957-87-1
分子式	C₃₂H₂₃ClF₃N₇O₄
分子量	662.02
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	EGFR-IN-8 是 EGFR 和 c-Met 双重抑制剂，化合物 48。EGFR-IN-8 有望成为进一步开发靶向 EGFR TKI 抗性 NSCLC 药物的靶点。
生物活性	EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.
性状	Solid
IC50 & Target[1][2]	EGFR; c-Met
体外研究(In Vitro)	EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97?cells at different time intervals, with IC50 values ranging from 0.3 to 0.6?μM and 0.2-0.5?μM after 48 and 72?h of treatment respectively. EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	EGFR-IN-8 (oral gavage; 50 and 150?mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150?mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Dokla EME, et al. 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. Eur J Med Chem. 2019 Aug 9;182:111607.

溶解度数据	In Vitro: DMSO : 8.33 mg/mL (12.58 mM; Need ultrasonic)配制储备液

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