Gefitinib-based PROTAC® 3

Tocris Bioscience | Catalog # 7258

Potent EGFR PROTAC® Degrader
Tocris Bioscience

Key Product Details

Description

Potent EGFR PROTAC® Degrader

Alternative Names

Iressa-based PROTAC 3
View all Active Degraders »

Product Description

Gefitinib-based PROTAC® 3 is a potent EGFR PROTAC® Degrader. Comprises an EGFR inhibitor gefitinib (Iressa Cat. No. 3000) conjugated to a VHL ligand via a linker. Induces EGFR degradation (DC50 values are 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively). Exhibits no degradation of wild-type EGFR at concentrations up to 10 μM.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Product Specifications for Gefitinib-based PROTAC® 3

Molecular Weight

934.52

Formula

C47H57ClFN7O8S

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

CAS Number

2230821-27-7

PubChem ID

135156947

InChI Key

NICKHWYZMNLEPJ-TZSMONEZSA-N

SMILES

COC1=CC2=C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)C=C1OCCCCCOCCOCCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 93.45 100

Preparing Stock Solutions for Gefitinib-based PROTAC® 3

The following data is based on the product molecular weight 934.52.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.07 mL 5.35 mL 10.70 mL
5 mM 0.21 mL 1.07 mL 2.14 mL
10 mM 0.11 mL 0.54 mL 1.07 mL
50 mM 0.02 mL 0.11 mL 0.21 mL

Calculators

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Background References

References are publications that support the biological activity of the product.

Product Documents for Gefitinib-based PROTAC® 3

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for Gefitinib-based PROTAC® 3

For research use only

Citations for Gefitinib-based PROTAC® 3

Customer Reviews for Gefitinib-based PROTAC® 3 (1)

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  • Not Published yet
    Name: Akanksha Patel
    Species: Mouse
    Assay Type: In Vivo
    Cell Line/Tissue: A549
    Verified Customer | Posted 12/04/2023
    Preparation of nanoformulation and tested in animals and different lung cancer cell lines.

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