Gefitinib-based PROTAC 3
Modify Date: 2024-01-07 00:07:31
Gefitinib-based PROTAC 3 structure
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Common Name | Gefitinib-based PROTAC 3 | ||
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| CAS Number | 2230821-27-7 | Molecular Weight | 934.51 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C47H57ClFN7O8S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Gefitinib-based PROTAC 3Gefitinib-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]. |
| Name | Gefitinib-based PROTAC 3 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
EGFR:11.7 nM (DC50, HCC827(exon 19 del) cells) EGFR:22.3 nM (DC50, H3255 (L858R mutantion) cells) PROTAC |
| 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]. Western Blot Analysis[1] Cell Line: HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR Concentration: 100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cells Incubation Time: 24 hours Result: Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation. |
| References |
| Molecular Formula | C47H57ClFN7O8S |
|---|---|
| Molecular Weight | 934.51 |
| Storage condition | 2-8℃ |