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PROTAC EGFR degrader 12

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Catalog No. T211103Cas No. 2654821-05-1

PROTACEGFRdegrader 12 (example 1) is a PROTAC degrader that selectively targets and degrades mutant EGFR, with minimal effect on EGFRWT. It demonstrates an IC50 of less than 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells).

PROTAC EGFR degrader 12

PROTAC EGFR degrader 12

😃Good
Catalog No. T211103Cas No. 2654821-05-1
PROTACEGFRdegrader 12 (example 1) is a PROTAC degrader that selectively targets and degrades mutant EGFR, with minimal effect on EGFRWT. It demonstrates an IC50 of less than 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells).
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Bioactivity
Description
PROTACEGFRdegrader 12 (example 1) is a PROTAC degrader that selectively targets and degrades mutant EGFR, with minimal effect on EGFRWT. It demonstrates an IC50 of less than 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells).
In vitro
PROTAC EGFR degrader 12 (example 1) exhibits growth inhibitory effects on Ba/F3 cell lines expressing both EGFR WT and mutants, with CTG 50 values of 1.62 μM for EGFR WT and 5-21 nM for EGFR mutants.
Chemical Properties
Molecular Weight931.02
FormulaC48H48F2N10O6S
Cas No.2654821-05-1
SmilesC(CC1(O)CCN(CC1)C2=C(F)C=C(N[C@@H]3C(=O)NC(=O)CC3)C=C2)(=O)N4CC5(CN(C5)C6=CC=C(C=C6)C=7C=C8C(=C(F)C7)CN(C(C(NC9=NC=CS9)=O)C%10=C%11N(C=N%10)CCC%11)C8=O)C4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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