1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Autophagy
  2. PROTACs EGFR Autophagy
  3. PROTAC EGFR degrader 4

PROTAC EGFR degrader 4 是一种有效的 PROTAC 靶向突变 EGFR。PROTAC EGFR degrader 4 诱导 EGFRdel19EGFRL858R/T790M 降解,DC50 值分别为 0.51 和 126 nM。PROTAC EGFR degrader 4 显着抑制 HCC827 和 H1975 细胞系的生长,IC50 值分别为 0.83 和 203.1 nM。诱导 EGFR 降解与自噬 (autophagy) 有关。

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PROTAC EGFR degrader 4 Chemical Structure

PROTAC EGFR degrader 4 Chemical Structure

CAS No. : 2882845-50-1

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy[1].

体外研究
(In Vitro)

PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFRdel19) and H1975 (EGFRL858R/T790M) with IC50s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively[1].
PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFRdel19 degradation with a DC50 values of 0.51 nM[1].
PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines[1].
PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

995.29

Formula

C55H70N12O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PROTAC EGFR degrader 4
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HY-146349
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