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).
In Vitro

Western Blot Analysis Cell Line:HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR Concentration:100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cells Incubation Time:24 hours Result:Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.
In Vivo

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Synonyms

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Pathway

PROTACs
Target

PROTAC
Recptor

PROTAC
Research Area

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Indication

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CAS Number

2230821-27-7
Formula Weight

934.522
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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