1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. PROTACs EGFR Apoptosis
  3. PROTAC EGFR degrader 5

PROTAC EGFR degrader 5 (Compound 10) 是一种 PROTAC EGFR 降解剂,可有效降解 HCC827 细胞中的 EGFRDel19DC50 为 34.8 nM。PROTAC EGFR degrader 5 显著诱导 HCC827 细胞凋亡 (apoptosis) 并将细胞阻滞在 G1 期。

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PROTAC EGFR degrader 5 Chemical Structure

PROTAC EGFR degrader 5 Chemical Structure

CAS No. : 2409793-36-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].

IC50 & Target

EGFR

34.8 nM (DC50)

体外研究
(In Vitro)

PROTAC EGFR degrader 5 (PROTAC 10, 0-10 μM approximately, 72 h) inhibits HCC827 cell (NSCLC cell) proliferation with an IC50 value of 0.22 μM[1].
PROTAC EGFR degrader 5 (1 nM-10 μM, 48 h or 4-96 h) concentration-dependently and time-dependently degrades EGFR with a DC50 value of 34.8 nM in HCC827 cells[1].
PROTAC EGFR degrader 5 (0.1-1 μM, 36 h) concentration-dependently inhibits EGFR and downstream Akt phosphorylation in HCC827 cells[1].
PROTAC EGFR degrader 5 (0.1-10 μM, 48 h) displays weak degradation activity on EGFR in H1975 and A549 cells[1].
PROTAC EGFR degrader 5 (0.1-1 μM, 32 h) dose-dependently induces the apoptosis of HCC827 cells and arrests the cells in G1 phase[1].

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

Cell Proliferation Assay[1]

Cell Line: HCC827, H1975, A549, A431
Concentration: 0-10 μM approximately
Incubation Time: 72 h
Result: Displayed more potent anti-proliferative activity against HCC827 cells than other cells, IC50 values: 0.22 μM (HCC827), > 10μM (H1975, A549, A431), respectively.

Western Blot Analysis[1]

Cell Line: HCC827 cell
Concentration: 1 nM-10 μM
Incubation Time: 48h for concentration-dependent assay, 4-96 h for time-dependent assay
Result: Degraded EGFR with a DC50 value of 34.8 nM in HCC827 cell in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HCC827 cell
Concentration: 0.1 μM, 1 μM
Incubation Time: 32 h
Result: Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HCC827 cell
Concentration: 0.1 μM, 1 μM
Incubation Time: 32 h
Result: Induced cell cycle arrest in G1 phase.
分子量

1070.33

Formula

C57H72FN13O5S

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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产品名称:
PROTAC EGFR degrader 5
目录号:
HY-146422
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