Description
K-Ras ligand-Linker Conjugate 5 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 5 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: 2378261-85-7
Molecular Weight: 789.96
Formula: C42H59N7O8
Chemical Name: tert-butyl (2S)-2-(cyanomethyl)-4-(2-{[(2S,4R)-4-(2-{2-[2-(2-hydroxyethoxy)ethoxy]ethoxy}ethoxy)-1-methylpyrrolidin-2-yl]methoxy}-7-(naphthalen-1-yl)-5H,6H,7H,8H-pyrido[3,4-d]pyrimidin-4-yl)piperazine-1-carboxylate
Smiles: CN1C[C@@H](C[C@H]1COC1N=C2CN(CCC2=C(N=1)N1C[C@H](CC#N)N(CC1)C(=O)OC(C)(C)C)C1C=CC=C2C=CC=CC2=1)OCCOCCOCCOCCO
InChiKey: YWJHMWJHKMFQGA-DHWXLLNHSA-N
InChi: InChI=1S/C42H59N7O8/c1-42(2,3)57-41(51)49-17-16-48(27-32(49)12-14-43)39-36-13-15-47(38-11-7-9-31-8-5-6-10-35(31)38)29-37(36)44-40(45-39)56-30-33-26-34(28-46(33)4)55-25-24-54-23-22-53-21-20-52-19-18-50/h5-11,32-34,50H,12-13,15-30H2,1-4H3/t32-,33-,34+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
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.
References:
- CREW, Andrew P., et al. MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE. WO2019195609A2.
Products are for research use only. Not for human use.
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