2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis
  4. Pro-PEG3-BA

Pro-PEG3-BA 是一种靶向 EML4-ALK/EGFR 的 PROTAC 降解剂，可分别以DC50 为 0.42 μM 和 13.50 μM 降解 EML4-ALK 与 EGFR 突变体 (L858R/T790M)。Pro-PEG3-BA 在体外实验中能够抑制非小细胞肺癌细胞的增殖，并诱导细胞发生周期阻滞与凋亡 (apoptosis)。Pro-PEG3-BA 具有良好的安全性特征，且在体内实验中可通过重新调控泛素-蛋白酶体系统降低 EML4-ALK 蛋白的表达水平。Pro-PEG3-BA 具备用于非小细胞肺癌的研究。

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Pro-PEG3-BA

Pro-PEG3-BA Chemical Structure

CAS No. : 3057939-64-4

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Pro-PEG3-BA 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research[1][2][3].

体外研究
(In Vitro)

Pro-PEG3-BA 在体外与纯化的 ALK 蛋白结合，Kd 为 387 nM[2]。Pro-PEG3-BA 在 HEK293T 细胞中与 GID4 蛋白结合，Kd 值为 6.05 μM[3]。
Pro-PEG3-BA (0-20 μM, 48 小时) 在 H3122 (EML4-ALK) 细胞中特异性降解 EML4-ALK 融合蛋白，对野生型或突变型 ALK 无影响[3]。
Pro-PEG3-BA (48-72 小时) 抑制细胞生长，对 H3122 细胞 (EML4-ALK) (48 小时) 的 IC50 值为 0.16 μM，对 H1975 细胞 (EGFR-L858R/T790M) (72 小时) 的 IC50 值为 8.8 μM，且对正常细胞 (HEK293T细胞) 毒性很小[3]。
Pro-PEG3-BA (10 μM, 24 小时) 显著下调 ALK 蛋白丰度，同时下调 CD2AP、MRPS23、RNF2、RAB18 和TRMT10C，证明其在靶向 ALK 降解方面具有高选择性；同时，在 H1975 (EGFR L858R/T790M) 细胞中上调 POLR2F、WASHC2C、NCOR2、ZNF622、ALDH6A1、PRRC1、GPD1L、EXOC7、WACPAF1[3]。
Pro-PEG3-BA (10-20 μM, 0-24 小时) 在 H3122 (EML4-ALK) (10 μM) 和 H1975 (EGFR-L858R/T790M) (20 μM) 细胞中以时间依赖性方式诱导 EML4-ALK 或 EGFR 突变蛋白明显减少[3]。
Pro-PEG3-BA (0.5-20 μM, 6 或 12 小时) 在 H3122 (EML4-ALK) 和 H1975 (EGFR-L858R/T790M) 细胞中以蛋白酶体依赖性方式降低 EML4-ALK 和 EGFR 突变体的水平[3]。
Pro-PEG3-BA (5-10 μM, 48-72 小时) 在 H1975 (EGFR-L858R/T790M) 细胞和 H3122 (EML4-ALK) 细胞中诱导细胞周期阻滞和细胞凋亡[3]。

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

Pro-PEG3-BA 相关抗体:

Western Blot Analysis [3]

Cell Line: H3122 cells (EML4-ALK), SK-N-BE(2) (express wild type ALK, and SH-SY5Y) and SH-SY5Y (harbors the ALK-F1174L)
Concentration: 0, 0.01, 0.1, 1, 10 and 20 μM
Incubation Time: 48 h
Result: Led to a noticeable downregulation of the EML4-ALK protein in H3122 (EML4-ALK) cells.
Did not affect the protein levels of either wild-type or mutant ALK.

Western Blot Analysis [3]

Cell Line: H3122 cells (EML4-ALK) and H1975 (EGFR L858R/T790M) cells
Concentration: 0.5 or 20 μM
Incubation Time: 6 h and 12 h
Result: Mediated the degradation of EML4-ALK or EGFR mutant, which was blocked by the proteasome inhibitor MG132 (HY-13259) (10 μM) instead of lysosome inhibitor Chloroquine (HY-17589A) (25 μM).

Western Blot Analysis [3]

Cell Line: H3122 (10 μM) and H1975 (20 μM )
Concentration: H3122 (10 μM) and H1975 (20 μM)
Incubation Time: 0, 12, 24, 36, 48 and 72 h
Result: Induced the apparent reduction of EML4-ALK or EGFR mutant proteins, with effects observed around 45 min and 12 h.

Cell Cycle Analysis [3]

Cell Line: H3122 cells (EML4-ALK) and H1975 (EGFR L858R/T790M) cells
Concentration: 5 or 10 μM
Incubation Time: 48 (for H3122 cells) or 72 h (for H1975 cells)
Result: Induced an accumulation of cells in the G1 phase and concurrently causing a decrease in the number of cells in the S or G2 phase.
Significantly increased the proportion of both early and late apoptotic cells in a concentration-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[3] 2 mg/kg i.v. Tmax 0.083 h
Mice[3] 50 mg/kg i.p. Tmax 0.5 h
Mice[3] 2 mg/kg i.v. T1/2 2.873 h
Mice[3] 50 mg/kg i.p. T1/2 5.175 h
Mice[3] 2 mg/kg i.v. Cmax 3.720 μg/mL
Mice[3] 50 mg/kg i.p. Cmax 33.010 μg/mL
Mice[3] 2 mg/kg i.v. AUC0-t 6.084 μg·h/mL
Mice[3] 50 mg/kg i.p. AUC0-t 80.849 μg·h/mL
Mice[3] 50 mg/kg i.p. F 53.21 %
体内研究
(In Vivo)

Pro-PEG3-BA (10 mg/kg，腹腔注射，隔日给药 1 次，总计给药 8 次) 在 H3122 细胞诱导的异种移植瘤小鼠模型中可显著降低 EML4-ALK 蛋白的表达水平，且具有良好的安全性特征[3]。

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

Animal Model: H3122 cells induced-female nude mice[3]
Dosage: 10 mg/kg
Administration: i.p., every other day for a total of 8 doses
Result: Did not cause significant variations in the mice body weight.
Decreased EML4-ALK protein levels in tumors.
分子量

787.28

Formula

C37H52ClN8O7P
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

Pro-PEG3-BA 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Pro-PEG3-BA3057939-64-4PROTACsAnaplastic lymphoma kinase (ALK)EGFRApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Epidermal growth factor receptorErbB-1HER1non-small cell lung cancerH3122EML4 ALKH1975NSCLCInhibitorinhibitorinhibit

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