A PROTAC that drives mutant EGFR degradation
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Gefitinib-based PROTAC 3

Item No. 28597

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
2230821-27-7
Synonyms
  • Gefitinib-based Proteolysis-targeting Chimera 3
Molecular Formula
C47H57ClFN7O8S
Formula Weight
934.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 16 mg/mlEthanol: 10 mg/ml
λmax
252, 332 nm
SMILES
ClC1=CC(NC2=NC=NC3=C2C=C(OCCCCCOCCOCCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)C(OC)=C3)=CC=C1F
InChi Code
InChI=1S/C47H57ClFN7O8S/c1-29-42(65-28-53-29)31-11-9-30(10-12-31)25-50-45(59)38-22-33(57)26-56(38)46(60)43(47(2,3)4)55-41(58)15-18-63-20-19-62-16-7-6-8-17-64-40-23-34-37(24-39(40)61-5)51-27-52-44(34)54-32-13-14-36(49)35(48)21-32/h9-14,21,23-24,27-28,33,38,43,57H,6-8,15-20,22,25-26H2,1-5H3,(H,50,59)(H,55,58)(H,51,52,54)/t33-,38+,43-/m1/s1
InChi Key
NICKHWYZMNLEPJ-TZSMONEZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).1 In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burslem, G.M., Smith, B.E., Lai, A.C., et al. The advantages of targeted protein degradation over inhibition: An RTK case study. Cell Chem. Biol. 25(1), 66-77 (2018).