Gefitinib-based PROTAC® 3

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Cat.No. 7258 - Gefitinib-based PROTAC® 3 | C47H57ClFN7O8S | CAS No. 2230821-27-7
Description: Potent EGFR PROTAC®
Alternative Names: Iressa-based PROTAC 3
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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity for Gefitinib-based PROTAC® 3

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.

Technical Data for Gefitinib-based PROTAC® 3

M. Wt 934.52
Formula C47H57ClFN7O8S
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Gefitinib-based PROTAC® 3

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 will 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 10.7 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

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Product Datasheets for Gefitinib-based PROTAC® 3

References for Gefitinib-based PROTAC® 3

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

Burslem et al (2018) The advantages of targeted protein degradation over inhibition: an RTK case study. Cell Chem.Biol. 25 67 PMID: 29129716


If you know of a relevant reference for Gefitinib-based PROTAC® 3, please let us know.

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Citations for Gefitinib-based PROTAC® 3

Citations are publications that use Tocris products.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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