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Gefitinib-based PROTAC 3
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Gefitinib-based PROTAC 3
Catalog No. T5437Cas No. 2230821-27-7
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $45 | In Stock | |
| 2 mg | $64 | In Stock | |
| 5 mg | $97 | In Stock | |
| 10 mg | $178 | In Stock | |
| 25 mg | $297 | In Stock | |
| 50 mg | $453 | In Stock | |
| 100 mg | $655 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1]. |
| In vitro | H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM; 24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR[1]. |
| Molecular Weight | 934.51 |
| Formula | C47H57ClFN7O8S |
| Cas No. | 2230821-27-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||
| Solubility Information | DMSO: 10 mM | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
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