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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COA HNMR HPLC

Gefitinib-based PROTAC 3

Catalog No. T5437Cas No. 2230821-27-7

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Pack Size	Price	Availability
2 mg	$38	In Stock
5 mg	$58	In Stock
10 mg	$107	In Stock
25 mg	$178	In Stock
50 mg	$272	In Stock
100 mg	$393	In 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 Weight	934.51
Formula	C₄₇H₅₇ClFN₇O₈S
Cas No.	2230821-27-7

Storage & Solubility Information

Storage

Powder: -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

	1mg	5mg	10mg	50mg
1 mM	1.0701 mL	5.3504 mL	10.7008 mL	53.5040 mL
5 mM	0.2140 mL	1.0701 mL	2.1402 mL	10.7008 mL
10 mM	0.1070 mL	0.5350 mL	1.0701 mL	5.3504 mL

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