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].
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 10,500 | |||
2 mg | 在庫あり | ¥ 15,000 | |||
5 mg | 在庫あり | ¥ 22,500 | |||
10 mg | 在庫あり | ¥ 41,000 | |||
25 mg | 在庫あり | ¥ 68,500 | |||
50 mg | 在庫あり | ¥ 104,000 | |||
100 mg | 在庫あり | ¥ 150,500 |
説明 | 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]. |
ターゲット&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]. |
分子量 | 934.51 |
分子式 | 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