Gefitinib-based PROTAC 3

Catalog No.S0070 Batch:S007003

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Technical Data

Formula
C47H57ClFN7O8S
Molecular Weight 934.51 CAS No. 2230821-27-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (107.0 mM)
Ethanol 100 mg/mL (107.0 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.625mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.
Targets
EGFR [1]
(in HCC827(Exon 19 del) cells)		 EGFR [1]
(in H3255 (L858R) cells)
11.7 nM(DC50) 22.3 nM(DC50)

Protocol (from reference)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.