Gefitinib-based PROTAC 3

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

基于吉非替尼的 PROTAC 3 是一种 VHL 招募 PROTAC，可诱导 EGFR 和 EGFR 突变体的降解，对于 HCC827 细胞（外显子 19 del）和 H3255 细胞（L858R）的 DC50 分别为 11.7 nM 和 22.3 nM。

Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).

Western Blot Analysis Cell Line:HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR Concentration:100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cells Incubation Time:24 hours Result:Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.

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PROTACs

PROTAC

PROTAC

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2230821-27-7

934.522

C47H57ClFN7O8S

>98% (HPLC)

DMSO : ≥ 60 mg/mL64.20 mM

CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O

(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years