K-Ras ligand-Linker Conjugate 6

• CAT Number: I015516
• CAS Number: 2378261-89-1
• Molecular Formula: C42H60N8O7
• Molecular Weight: 788.98
• Purity: ≥95%
• Synonyms: tert-butyl (2S)-4-[2-[[(2S,4R)-4-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]-1-methylpyrrolidin-2-yl]methoxy]-7-naphthalen-1-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-2-(cyanomethyl)piperazine-1-carboxylate
• InChI: InChI=1S/C42H60N8O7/c1-42(2,3)57-41(51)50-18-17-49(27-32(50)12-14-43)39-36-13-16-48(38-11-7-9-31-8-5-6-10-35(31)38)29-37(36)45-40(46-39)56-30-33-26-34(28-47(33)4)55-25-24-54-23-22-53-21-20-52-19-15-44/h5-11,32-34H,12-13,15-30,44H2,1-4H3/t32-,33-,34+/m0/s1
• InChIKey: BESPBPQQMBNUCA-DHWXLLNHSA-N
• SMILES: CC(C)(C)OC(=O)N1CCN(CC1CC#N)C2=NC(=NC3=C2CCN(C3)C4=CC=CC5=CC=CC=C54)OCC6CC(CN6C)OCCOCCOCCOCCN

K-Ras ligand-Linker Conjugate 6 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 6 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.