Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 45.00 | |
2 mg | In stock | $ 64.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 178.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 453.00 | |
100 mg | In stock | $ 655.00 |
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]. |
Targets&IC50 | EGFR:11.7 nM (DC50, HCC827(exon 19 del) cells), EGFR:22.3 nM (DC50, H3255 (L858R mutantion) cells) |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
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Gefitinib-based PROTAC 3 2230821-27-7 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Epidermal growth factor receptor inhibit Inhibitor Gefitinib based PROTAC 3 HER1 PROTACs ErbB-1 Gefitinibbased PROTAC 3 inhibitor