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Gefitinib-based PROTAC 3

Name: Gefitinib-based PROTAC 3
Brand: TargetMol
SKU: T5437
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

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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].

Gefitinib-based PROTAC 3

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Purity: 98.25%

Catalog No. T5437Cas No. 2230821-27-7

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$38	In Stock	In Stock
5 mg	$58	In Stock	In Stock
10 mg	$107	In Stock	In Stock
25 mg	$178	In Stock	In Stock
50 mg	$272	-	In Stock
100 mg	$393	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:98.25%

Appearance:Solid

Color:White

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COA HNMR HPLC

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:22.3 nM (DC50, H3255 (L858R mutantion) cells), EGFR:11.7 nM (DC50, HCC827(exon 19 del) 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
Smiles	N(C=1C2=C(C=C(OC)C(OCCCCCOCCOCCC(N[C@H](C(=O)N3[C@H](C(NCC4=CC=C(C=C4)C=5SC=NC5C)=O)C[C@@H](O)C3)[C@](C)(C)C)=O)=C2)N=CN1)C6=CC(Cl)=C(F)C=C6
Relative Density.	1.300 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mM, Sonication is recommended.

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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc