K-Ras ligand-Linker Conjugate 4

• CAT Number: I016930
• CAS Number: 2378261-83-5
• Molecular Formula: C35H51N7O8
• Molecular Weight: 697.82
• Purity: ≥95%
• Synonyms: benzyl (2S)-2-(cyanomethyl)-4-[2-[[(2S,4R)-4-[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethoxy]-1-methylpyrrolidin-2-yl]methoxy]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl]piperazine-1-carboxylate
• InChI: InChI=1S/C35H51N7O8/c1-40-24-30(48-20-19-47-18-17-46-16-15-45-14-13-43)21-29(40)26-49-34-38-32-22-37-10-8-31(32)33(39-34)41-11-12-42(28(23-41)7-9-36)35(44)50-25-27-5-3-2-4-6-27/h2-6,28-30,37,43H,7-8,10-26H2,1H3/t28-,29-,30+/m0/s1
• InChIKey: GUKYSZDGLMYSDL-OIFRRMEBSA-N
• SMILES: CN1CC(CC1COC2=NC3=C(CCNC3)C(=N2)N4CCN(C(C4)CC#N)C(=O)OCC5=CC=CC=C5)OCCOCCOCCOCCO

K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

Reference

[1]. CREW, Andrew P., et al. MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE. WO2019195609A2.