Description
The covalent PROTAC CP17, with a novel purine-containing EGFR ligand, as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. The CP17 exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity.
Product information
Molecular Weight: 1092.40
Formula: C60H77N13O5S
Chemical Name: (2S, 4R)-1-[(2S)-3, 3-dimethyl-2-{8-[4-(4-{[8-(phenylamino)-9-[(3S)-1-(prop-2-enoyl)piperidin-3-yl]-9H-purin-2-yl]amino}phenyl)piperazin-1-yl]octanamido}butanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
Smiles: CC1N=CSC=1C1C=CC(=CC=1)[C@H](C)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)CCCCCCCN1CCN(CC1)C1C=CC(=CC=1)NC1=NC2=C(C=N1)N=C(NC1C=CC=CC=1)N2[C@@H]1CN(CCC1)C(=O)C=C)C(C)(C)C
InChiKey: RYXQXEGTLNBKEC-DKQRTKIFSA-N
InChi: InChI=1S/C60H77N13O5S/c1-7-52(76)71-30-16-19-47(37-71)73-55-49(66-59(73)65-44-17-12-11-13-18-44)36-61-58(68-55)64-45-25-27-46(28-26-45)70-33-31-69(32-34-70)29-15-10-8-9-14-20-51(75)67-54(60(4,5)6)57(78)72-38-48(74)35-50(72)56(77)63-40(2)42-21-23-43(24-22-42)53-41(3)62-39-79-53/h7,11-13,17-18,21-28,36,39-40,47-48,50,54,74H,1,8-10,14-16,19-20,29-35,37-38H2,2-6H3,(H,63,77)(H,65,66)(H,67,75)(H,61,64,68)/t40-,47-,48+,50-,54+/m0/s1
Technical Data
Purity: ≥95% (or refer to the Certificate of Analysis)
Shelf Life: ≥12 months if stored properly.
Products are for research use only. Not for human use.
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