EGFR-IN-8

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EGFR-IN-8 可能是进一步开发针对 EGFR TKI 耐药 NSCLC 的有希望的候选化合物。 EGFR-IN-8 是一种 EGFR 和 c-Met 双重抑制剂。

EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC. EGFR-IN-8 is a dual EGFR and c-Met inhibitor.(In Vitro):In A549, PC9, H1975, CL68, and CL97?cells, 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. EGFR-IN-8 (0-20 μM; 24, 48, 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.(In Vivo):EGFR-IN-8 (50,150?mg/kg; oral gavage) exhibits suppression (29% and 60%, respectively) of H1975 xenograft tumor growth in a dose-dependent manner.

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. Cell Viability Assay Cell Line:A549, PC9, H1975, CL68, and CL97?cells Concentration:0-20 μM Incubation Time:24 hours, 48 hours, 72 hours Result:Showed inhibitory effects on different cells.Western Blot Analysis Cell Line:A549, PC9, H1975, CL68, and CL97?cells Concentration:0-0.6 μM Incubation Time:48 hours Result:Decreased EGFR and c-Met expression.

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. Animal Model:Nude mice H1975 xenograft tumor model Dosage:50 and 150?mg/kg Administration:Oral gavage; 50 and 150?mg/kg; once daily; 20 days Result:Inhibited H1975 xenograft tumor growth.

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Angiogenesis

EGFR

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2407957-87-1

662.03

C32H23ClF3N7O4

>98% (HPLC)

In Vitro:?DMSO : 8.33 mg/mL (12.58 mM)

FC(F)(F)c1cc(NC(=O)Nc2cccc(c2)-c2nc(no2)-c2ccc(NC(=O)c3cccnc3)cc2Cl)ccc1NC(=O)C1CC1

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(-20℃)

With Ice Pack

≥ 2 years