PROTAC EGFR degrader 9_product_DataBase

Bioactivity	PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537))[1].
Invitro	PROTAC EGFR degrader 9（化合物 C6）针对 EGFRDel19/T790M/C797S、EGFRL858R/T790M、EGFRDel19 和 EGFRWT 的 DC50 分别为 36.5、88.5、75.4 和 >300 nM[1]。 PROTAC EGFR degrader 9（1.2-300 nM；24 小时）以剂量依赖性方式降解 H1975-TM 细胞中的 EGFRL858R/T790M/C797S 蛋白[1]。PROTAC EGFR degrader 9 对 PC-9-TMb（含有 EGFRDel19/T790M/C797S）、H1975、PC-9 和 A549 细胞表现出显着的抑制作用，IC50 值分别为 43.5 nM、46.2 nM、17.5 nM 和 97.5 nM[1]。PROTAC EGFR degrader 99（5-20 nM；24 小时）将 H1975-TM 细胞阻滞于 G0/G1 期，并以浓度依赖性方式促进细胞凋亡[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PROTAC EGFR degrader 9 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	PROTAC EGFR degrader 9 （Compound C6；25-100 mg/kg；口服；每日一次；持续31天）显着降低肿瘤组织中 EGFR 蛋白水平，抑制 EGFR 磷酸化，阻断下游信号通路的激活[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
Formula	C45H48F3N9O6S
Molar Mass	899.98
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yasheng Zhu, et al. Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation. J Med Chem. 2024 May 9;67(9):7283-7300.

PeptideDB

PROTAC EGFR degrader 9

CAS: F: C45H48F3N9O6S W: 899.98