2. PROTAC Apoptosis Protein Tyrosine Kinase/RTK
  3. PROTACs Apoptosis Anaplastic lymphoma kinase (ALK)
  4. PROTAC EML4-ALK Degrader-1

PROTAC EML4-ALK Degrader-1  (Synonyms: Pro-BA)

目录号: HY-174368
产品使用指南 技术支持

PROTAC EML4-ALK Degrader-2 (Pro-BA) 是一种具有选择性和口服有效的无连接子的 EML4-ALK PROTAC 降解剂，在 H1322 细胞中的 DC50 为 74 nM，T1/2 为 8 h。PROTAC EML4-ALK Degrader-2 依赖于 GID4 和蛋白酶体途径促进靶蛋白的泛素化，导致细胞凋亡apoptosis。PROTAC EML4-ALK Degrader-2 可用于癌症的研究。(粉色: EML4-ALK 配体 (HY-40114); 蓝色: GID4 配体 (HY-150908))

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PROTAC EML4-ALK Degrader-1

PROTAC EML4-ALK Degrader-1 Chemical Structure

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PROTAC EML4-ALK Degrader-1 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC50 of 74 nM in H1322 cells (T1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer. (Pink: EML4-ALK Ligand (HY-40114); Blue: GID4 Ligand (HY-150908)) [1]

体外研究
(In Vitro)

PROTAC EML4-ALK Degrader-2 (Compound Pro-BA) (0-1 μM; 0-24 小时) 可以显著和选择性地降解 EML4-ALK 的水平，并显著抑制 H3122(DC50 = 74 nM)、BaF3-EML4-ALK (DC50 = 125 nM) 和神经母细胞瘤 SK-N-BE(2) 细胞 (DC50 = 2.1 μM) 中细胞的生长[1]。
PROTAC EML4-ALK Degrader-2 (500 nM; 24 小时) 显著增加 H3122 细胞的细胞凋亡[1]。
PROTAC EML4-ALK Degrader-2 (500 nM; 24 小时) 通过泛素-蛋白酶体系统诱导 EML4-ALK 的降解[1]。

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

PROTAC EML4-ALK Degrader-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: H3122 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Increased the proportion of G1 phase cells.

Cell Viability Assay[1]

Cell Line: H3122 cells
Concentration: 0-1 μM
Incubation Time: 48 h
Result: Significantly inhibited the growth of H3122 cells (IC50 = 34 nM).

Apoptosis Analysis[1]

Cell Line: H3122 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Significantly increased the proportion of early and late apoptosis.
体内研究
(In Vivo)

PROTAC EML4-ALK Degrader-2 (Compound Pro-BA) (10 mg/kg; 腹腔注射; 每隔一天一次; 共 8 次) 在 H3122 异种移植肿瘤雌性裸鼠中显著降低 EML4-ALK 的水平并抑制肿瘤生长[1]。
PROTAC EML4-ALK Degrader-2 (25 mg/kg; 口服; 每两天一次; 共 8 次) 在 H3122 异种移植肿瘤雌性裸鼠中降低 EML4-ALK 的水平并抑制肿瘤生长，表现出低毒性[1]。

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

Animal Model: 1×107 H3122 cells injected female nude mice (4 weeks)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.); every other day for a total of 8 doses
Result: Significantly reduced the level of EML4-ALK protein in tumors.
Had good tolerance and no significant change in weight.
Significantly inhibits the volume of tumors.
Animal Model: 1×107 H3122 cells injected female nude mice (4 weeks)[1]
Dosage: 25 mg/kg
Administration: Oral administration (p.o.); every two days for a total of 8 doses
Result: Significantly reduced the level of EML4-ALK protein in tumors.
Significantly inhibits the volume of tumors.
Did not change the structure in the main organs.
分子量

584.05

Formula

C28H35ClN7O3P
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 EML4-ALK Degrader-1 相关分类

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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 EML4-ALK Degrader-1Pro-BAPROTACsApoptosisAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246EML4-ALKPROTACUbiquitinationCancerapoptosisH1322Inhibitorinhibitorinhibit

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