Gefitinib-based PROTAC 3 ( —— )

Catalog No. M13575 CAS No. 2230821-27-7

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Product Name

Gefitinib-based PROTAC 3
Note

Research use only, not for human use.
Brief Description

Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
Description

Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
Synonyms

——
Pathway

PROTACs
Target

PROTAC
Recptor

PROTAC
Research Area

——
Indication

——

CAS Number

2230821-27-7
Formula Weight

934.52
Molecular Formula

C47H57ClFN7O8S
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 60 mg/mL64.20 mM
SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O
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

1. Burslem GM, et al. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.

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