2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. PROTACs EGFR
  4. Gly-PEG3-BA

Gly-PEG3-BA 是一种靶向 EML4-ALK 的 PROTAC 降解剂。Gly-PEG3-BA 在 H3122 细胞 (EML4-ALK 阳性细胞) 中可有效降解 EML4-ALK 蛋白，其 DC50 为 0.50 μM；Gly-PEG3-BA 在 H1975 细胞 (EGFR L858R/T790M 双突变细胞) 中能显著降低 EGFR 突变体 (L858R/T790M) 的蛋白水平，对应的 DC50 值为 20.15 μM。此外，Gly-PEG3-BA 对 H3122 细胞与 H1975 细胞均具有强效抗增殖活性，其 IC50 分别为 0.84 μM 与 20.74 μM。Gly-PEG3-BA 可用于非小细胞肺癌的相关研究。

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Gly-PEG3-BA

Gly-PEG3-BA Chemical Structure

CAS No. : 3057939-66-6

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Gly-PEG3-BA 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research[1].

IC50 & Target[1]

EML4-ALK

 

体外研究
(In Vitro)

Gly-PEG3-BA (0-20 μM，72 小时) 在携带 EGFR L858R/T790M 双突变的 H1975 细胞中，表现出针对 EGFR 的高度靶向选择性活性，并在 H3122 (携带 EML4-ALK 融合基因) 细胞中诱导 EML4-ALK 融合蛋白发生剂量依赖性的靶向降解[1]。
Gly-PEG3-BA (0-20 μM，48 或 72 小时) 能有效下调 EML4-ALK 和 EGFR 突变体水平，并在 H3122 (EML4-ALK) 和 H1975 (EGFR-L858R/T790M) 细胞中赋予强大的抗增殖活性，其 IC50 值分别为 0.84 μM和 20.74 μM[1]。
Gly-PEG3-BA (0-20 μM，48 或 72 小时) 能在 H3122 和 H1975 细胞中，以剂量依赖的方式有效降低 EML4-ALK 或 EGFR 突变体蛋白水平[1]。
Gly-PEG3-BA 诱导 EML4-ALK 和突变型 EGFR 的降解，该降解过程在 H3122 和 H1975 细胞中由 ZYG11B 和 ZER1 介导 (通过敲低 ZYG11B 和 ZER 1表达证实) [1]。

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

Gly-PEG3-BA 相关抗体:

Western Blot Analysis[1]

Cell Line: H1975 (harboring the EGFR L858R/ T790M double mutation), A549, H1299, PC9, H3122 (EML4-ALK) cells
Concentration: 0, 0.01, 0.1, 1, 10 and 20 μM
Incubation Time: 72 h
Result: Triggered the degradation of EGFR without affecting the wild-type EGFR protein level in A549 and H1299 cells or the EGFR del19 mutant protein levels in PC9 cells.
Resulted an apparent downregulation of the EML4 ALK protein in H3122 cells at varying doses.

Western Blot Analysis[1]

Cell Line: H3122 (EML-ALK), H1975 (EGER-L858R/T790M) cells
Concentration: 0, 0.01, 0.1, 0.25, 0.5, 0.75, 1, 2.5, 5, 7.5, 10 μM, or 0, 10, 12.5, 15, 17.5 and 20 μM
Incubation Time: 48 (for H3122 cell) or 72 h (for H1975 cell)
Result: Effectively reduced EML4-ALK in H3122 (EML-ALK) cells, with a DC50 value of 0.50 μM, and attained a 98% reduction at ∼10 μM.
Effectively reduced EGFR levels with DC50 of 20.15 μM and achieved a 43% at around 20 μM in H1975 (EGER-L858R/T790M) cells.

Western Blot Analysis[1]

Cell Line: H3122 (EML-ALK), H1975 (EGER-L858R/T790M) cells
Concentration: 10 (for H3122) or 20 (for H1975) μM
Incubation Time: 0, 0.25, 0.75, 1.5, 3, 6, 12 and 24 h (for H3122) or 0, 12, 24, 36, 48 and 72 h (for H1975)
Result: led to a decrease in EML4-ALK or EGFR mutant protein levels at 15 min and 24 h.
分子量

747.22

Formula

C34H48ClN8O7P
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

Gly-PEG3-BA 相关分类

  • 摩尔计算器

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  • Do most proteins show cross-species activity?

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Keywords:

Gly-PEG3-BA3057939-66-6PROTACsEGFREpidermal growth factor receptorErbB-1HER1non-small lung cancer H3122 (EML4-ALK) cellsH1975 (L858R/T790M) cellsInhibitorinhibitorinhibit

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