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Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3
Gefitinib-based PROTAC 3, which connects 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 mutation) cells, respectively[1].
Catalog No. T5437Cas No. 2230821-27-7
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Purity:98.25%
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Gefitinib-based PROTAC 3

Catalog No. T5437Cas No. 2230821-27-7
Gefitinib-based PROTAC 3, which connects 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 mutation) cells, respectively[1].
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2 mg$38In Stock
5 mg$58In Stock
10 mg$107In Stock
25 mg$178In Stock
50 mg$272In Stock
100 mg$393In Stock
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Product Introduction

Bioactivity
Description
Gefitinib-based PROTAC 3, which connects 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 mutation) 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].
Chemical Properties
Molecular Weight934.51
FormulaC47H57ClFN7O8S
Cas No.2230821-27-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 10 mM
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.0701 mL5.3504 mL10.7008 mL53.5040 mL
5 mM0.2140 mL1.0701 mL2.1402 mL10.7008 mL
10 mM0.1070 mL0.5350 mL1.0701 mL5.3504 mL

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