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 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)).

For research use only. We do not sell to patients.

PROTAC EGFR degrader 15

PROTAC EGFR degrader 15 Chemical Structure

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Based on 1 publication(s) in Google Scholar

PROTAC EGFR degrader 15 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

In Vitro

PROTAC EGFR degrader 15 (Compound P-G) (0-1 μM, 24 h + washout 0-72 h) effectively and sustainably induces EGFR protein degradation via both ubiquitin/proteasome pathway and autophagy/lysosome degradation pathway both in HCC-827 parental and EGFR-tyrosine kinase inhibitors (EGFR-TKIs) resistant cells[1].
PROTAC EGFR degrader 15 (0.5 μM, 44-64°C, 2 h) promotes energy production in HCC-827-ER (Erlotinib (HY-50896) resistance) resistance cells by targeting ETFA[1].

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

PROTAC EGFR degrader 15 Related Antibodies

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.
In Vivo

PROTAC EGFR degrader 15 (Compound P-G) (30 mg/kg, i.p., every other day for 2 weeks) effectively suppresses HCC-827-GR xenografts tumors in mice[1].

MedChemExpress (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 %.
Was no statistical differences in organ indices between vehicle treated group.
Molecular Weight

871.40

Formula

C45H52ClFN8O7
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1)CCC(N2C(C(C(NC(CCCCCCCCCN3CCN(CCCOC4=CC(C(NC5=CC(Cl)=C(F)C=C5)=NC=N6)=C6C=C4OC)CC3)=O)=CC=C7)=C7C2=O)=O)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (114.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1476 mL 5.7379 mL 11.4758 mL
5 mM 0.2295 mL 1.1476 mL 2.2952 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1476 mL 5.7379 mL 11.4758 mL 28.6895 mL
5 mM 0.2295 mL 1.1476 mL 2.2952 mL 5.7379 mL
10 mM 0.1148 mL 0.5738 mL 1.1476 mL 2.8689 mL
15 mM 0.0765 mL 0.3825 mL 0.7651 mL 1.9126 mL
20 mM 0.0574 mL 0.2869 mL 0.5738 mL 1.4345 mL
25 mM 0.0459 mL 0.2295 mL 0.4590 mL 1.1476 mL
30 mM 0.0383 mL 0.1913 mL 0.3825 mL 0.9563 mL
40 mM 0.0287 mL 0.1434 mL 0.2869 mL 0.7172 mL
50 mM 0.0230 mL 0.1148 mL 0.2295 mL 0.5738 mL
60 mM 0.0191 mL 0.0956 mL 0.1913 mL 0.4782 mL
80 mM 0.0143 mL 0.0717 mL 0.1434 mL 0.3586 mL
100 mM 0.0115 mL 0.0574 mL 0.1148 mL 0.2869 mL
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PROTAC EGFR degrader 15 Related Classifications

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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