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.

Product information

CAS Number: 2378261-83-5

Molecular Weight: 697.82

Formula: C35H51N7O8

Chemical Name: benzyl (2S)-2-(cyanomethyl)-4-(2-{[(2S,4R)-4-(2-{2-[2-(2-hydroxyethoxy)ethoxy]ethoxy}ethoxy)-1-methylpyrrolidin-2-yl]methoxy}-5H,6H,7H,8H-pyrido[3,4-d]pyrimidin-4-yl)piperazine-1-carboxylate

Smiles: CN1C[C@@H](C[C@H]1COC1N=C2CNCCC2=C(N=1)N1C[C@H](CC#N)N(CC1)C(=O)OCC1C=CC=CC=1)OCCOCCOCCOCCO

InChiKey: GUKYSZDGLMYSDL-OIFRRMEBSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

Products are for research use only. Not for human use.