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PROTACEGFRdegrader 15 is a bifunctional EGFR PROTAC degrader composed of Pomalidomide and Gefitinib. It facilitates EGFR degradation through ubiquitin-proteasome dependent proteolysis and autophagic-lysosomal pathways. Additionally, PROTACEGFRdegrader 15 targets ETFA to enhance ATP production. It significantly suppresses tumor growth in Gefitinib-resistant HCC-827 xenograft models.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PROTACEGFRdegrader 15 is a bifunctional EGFR PROTAC degrader composed of Pomalidomide and Gefitinib. It facilitates EGFR degradation through ubiquitin-proteasome dependent proteolysis and autophagic-lysosomal pathways. Additionally, PROTACEGFRdegrader 15 targets ETFA to enhance ATP production. It significantly suppresses tumor growth in Gefitinib-resistant HCC-827 xenograft models. |
| In vitro | PROTAC EGFR degrader 15 (Compound P-G) effectively and persistently induces degradation of the EGFR protein in HCC-827 parent cells and EGFR tyrosine kinase inhibitor (EGFR-TKIs) resistant cells via the ubiquitin-proteasome and autophagy-lysosome pathways when used at 0-1 μM for 24 hours with elution from 0-72 hours. Additionally, at 0.5 μM and 44-64°C for 2 hours, it targets ETFA to promote energy production in HCC-827-ER (Erlotinib-resistant) cells. |
| In vivo | PROTAC EGFR degrader 15 (Compound P-G) administered at a dose of 30 mg/kg via intraperitoneal injection every other day for two weeks effectively inhibited the growth of HCC-827-GR xenografts in mice. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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