2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs EGFR Apoptosis
  4. PROTAC EGFR degrader 6

PROTAC EGFR degrader 6 是一种 PROTAC EGFR 降解剂，可有效降解 HCC827 细胞中的 EGFRDel19，DC50 为 45.2 nM。PROTAC EGFR degrader 6 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 6 Chemical Structure

PROTAC EGFR degrader 6 Chemical Structure

CAS No. : 2409793-28-6

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PROTAC EGFR degrader 6 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].

IC50 & Target

IC50: 180 nM (EGFRDel19 in HCC827 cells)[1]
DC50: 45.2 nM (EGFRDel19 in HCC827 cells)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
> 10 μM
Compound: 2
Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
A549 IC50
> 10 μM
Compound: 2
Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
HCC827 IC50
0.18 μM
Compound: 2
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
NCI-H1975 IC50
> 10 μM
Compound: 2
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
体外研究
(In Vitro)

PROTAC EGFR degrader 6 (compound 2) (0.001-10 μM; 48 hours) exhibits potent EGFR degradation activity with certain concentration-dependent manner; and shows DC50 of 45.2 nM in HCC827 cells[1].
PROTAC EGFR degrader 6 (100 nM; 4-96 hours) degradates EGFR protein in a time-dependent manner, and reaches the maximum degradation rate (Dmax = 87%) at 96 h[1].
PROTAC EGFR degrader 6 (0.1, 1 and 10 μM; 48 hours) shows weak degradation activity on EGFR in H1975 and A549 cells[1].
PROTAC EGFR degrader 6 (0.1 and 1 μM; 32 hours) induce HCC827 apoptosis, and the percentages of apoptosis cells are 53.72% and 32.31% at 0.1 and 1 μM, respectively[1].

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

PROTAC EGFR degrader 6 相关抗体:
分子量

913.05

Formula

C49H57FN12O5
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

PROTAC EGFR degrader 6 相关分类

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  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

PROTAC EGFR degrader 62409793-28-6PROTAC EGFR degrader6PROTAC EGFR degrader-6PROTACsEGFRApoptosisEpidermal growth factor receptorErbB-1HER1EGFR-TKEGFR-TK degradersProteolysis targeting chimeraPROTAC strategyInhibitorinhibitorinhibit

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