TargetMol

Gefitinib-based PROTAC 3

Product Code:
 
TAR-T5437
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T5437-1mg1mg£107.00
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TAR-T5437-2mg2mg£122.00
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TAR-T5437-5mg5mg£148.00
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TAR-T5437-10mg10mg£213.00
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TAR-T5437-25mg25mg£309.00
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TAR-T5437-50mg50mg£434.00
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Quantity:
TAR-T5437-100mg100mg£597.00
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Quantity:
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Further Information

Bioactivity:
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].
CAS:
2230821-27-7
Formula:
C47H57ClFN7O8S
Molecular Weight:
934.52
Pathway:
Tyrosine Kinase/Adaptors; Angiogenesis; JAK/STAT signaling
Purity:
0.9825
SMILES:
COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCCCOCCOCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(cc1)-c1scnc1C)C(C)(C)C
Target:
EGFR

Documents

References

Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 201. Jan 18;25(1):67-77.e3.