A PROTAC that drives mutant EGFR degradation
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PROTAC EGFR Degrader-9

Item No. 45393

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-4-[4-[[4-[1-(ethylsulfonyl)-1H-indol3-yl]-5-(trifluoromethyl)-2-pyrimidinyl]amino]phenyl]-1-piperazineheptanamide
CAS Number
2992670-33-2
Synonyms
  • Proteolysis-targeting Chimera EGFR Degrader-9
  • Proteolysis-targeting Chimera Epidermal Growth Factor Receptor Degrader-9
Molecular Formula
C45H48F3N9O6S
Formula Weight
900.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC(F)(F)C(C(C(C1=CC=CC=C12)=CN2[S](CC)(=O)=O)=N3)=CN=C3NC4=CC=C(N(CC5)CCN5CCCCCCC(NC6=C(CN(C(CCC7=O)C(N7)=O)C8=O)C8=CC=C6)=O)C=C4
InChi Code
InChI=1S/C45H48F3N9O6S/c1-2-64(62,63)57-28-34(31-10-6-7-13-37(31)57)41-35(45(46,47)48)26-49-44(53-41)50-29-15-17-30(18-16-29)55-24-22-54(23-25-55)21-8-4-3-5-14-39(58)51-36-12-9-11-32-33(36)27-56(43(32)61)38-19-20-40(59)52-42(38)60/h6-7,9-13,15-18,26,28,38H,2-5,8,14,19-25,27H2,1H3,(H,51,58)(H,49,50,53)(H,52,59,60)
InChi Key
NFLKKMOHWZTOPF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    PROTAC EGFR degrader-9 is a proteolysis-targeting chimera (PROTAC) containing the mutant EGFRT790M/C797S-binding compound D51 conjugated to the cereblon (CRBN) ligand lenalidomide (Item No. 14643) via an alkyl linker.1 It selectively induces degradation of mutant EGFRs over wild-type EGFR with half-maximal degradation concentration (DC50) values of 10.2, 36.5, 88.5, 75.4, and >300 nM for EGFRL858R/T790M/C797S, EGFRΔ19/T790M/C797S, EGFRL858R/T790M, EGFRΔ19, and wild-type EGFR, respectively. PROTAC EGFR degrader-9 inhibits the growth of H1975 non-small cell lung cancer (NSCLC) cells expressing mutant EGFRL858R/T790M/C797S (IC50 = 10.3 nM) and induces cell cycle arrest at the G0/G1 phase and apoptosis in the same cells. It reduces tumor size in an H1975 xenograft mouse model when administered at doses of 25 and 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhu, Y., Ye, X., Wu, Y., et al. Design, synthesis, and biological evaluation of novel EGFR PROTACs targeting C797S mutation. J. Med. Chem. 67(9), 7283-7300 (2024).