2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Membrane Transporter/Ion Channel
  3. PROTACs EGFR ATP Synthase
  4. PROTAC EGFR degrader 15

PROTAC EGFR degrader 15 是一种基于 Pomalidomide (HY-10984) 和 Gefitinib (HY-50895) 的双功能 EGFR PROTAC 降解剂。PROTAC EGFR degrader 15 通过泛素-蛋白酶体依赖的蛋白水解和自噬-溶酶体活化途径触发 EGFR 降解。PROTAC EGFR degrader 15 靶向 ETFA 以增强 ATP 的产生。PROTAC EGFR degrader 15 显著抑制 Gefitinib 获得性耐药 HCC-827 异种移植模型中的肿瘤生长。PROTAC EGFR degrader 15 可用于非小细胞肺癌 (NSCLC) 的研究 (粉色：EGFR 配体 (HY-W109039)；蓝色：CRBN 配体 (HY-10984)；黑色：连接子 (HY-W679737))。

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PROTAC EGFR degrader 15

PROTAC EGFR degrader 15 Chemical Structure

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PROTAC EGFR degrader 15 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:

查看所有亚型
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 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737))[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

PROTAC EGFR degrader 15 (Compound P-G) (0-1 μM, 24 h + 洗脱 0-72 h) 可有效且持续地通过泛素/蛋白酶体途径和自噬/溶酶体降解途径诱导 HCC-827 亲本细胞和 EGFR 酪氨酸激酶抑制剂 (EGFR-TKIs) 耐药细胞中的 EGFR 蛋白降解[1]。
PROTAC EGFR degrader 15 (0.5 μM, 44-64°C, 2 h) 通过靶向 ETFA促进 HCC-827-ER (Erlotinib (HY-50896) 耐药) 耐药细胞的能量产生[1]。

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

PROTAC EGFR degrader 15 相关抗体:

Western Blot Analysis[1]

Cell Line: HCC-827, HCC-827-GR, HCC-827-ER, HCC-827-OR and HCC-827-RR cells
Concentration: 0, 0.1, 0.5 and 1 μM
Incubation Time: 24 h + washout 0, 6, 12, 24, 48 and 72 h
Result: Exhibited concentration-dependent and long lasting degradation of EGFR and p-EGFR in all cell lines.

Western Blot Analysis[1]

Cell Line: HCC-827 cells
Concentration: 0.5 μM
Incubation Time: 2 h
Result: Resulted in a significant increase in the thermal stability of ETFA at various temperatures both in intact cells.
体内研究
(In Vivo)

PROTAC EGFR degrader 15 (Compound P-G) (30 mg/kg，腹腔注射，每隔一天一次，共两周) 在小鼠上抑制了 HCC-827-GR 移植瘤的生长[1]。

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

Animal Model: HCC-827-GR xenografts model established in male BALB/c nude mice (20 g)[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.), every other day for 2 weeks
Result: Suppressed the HCC-827-GR xenografts tumor and the tumor growth inhibition (TGI) was 48.24 %.
Were no statistical differences in organ indices between vehicle treated group.
分子量

871.40

Formula

C45H52ClFN8O7
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 15 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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 15PROTAC EGFR degrader15PROTAC EGFR degrader-15PROTACsEGFRATP SynthaseEpidermal growth factor receptorErbB-1HER1NSCLCPROTACEGFR mutationEGFR-TKI acquired resistanceInhibitorinhibitorinhibit

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