K-Ras ligand-Linker Conjugate 1


Catalog No. Size PriceQuantity
M11601-2 Contact sales@xcessbio.com for quotation $100
M11601-10 Contact sales@xcessbio.com for quotation $100

Description

K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 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

Molecular Weight: 826.94

Formula: C43H54N8O9

Chemical Name: benzyl (2S)-2-(cyanomethyl)-4-(2-{[(2S, 4R)-4-[2-(2-{2-[2-(1, 3-dioxo-2, 3-dihydro-1H-isoindol-2-yl)ethoxy]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]1COC1=NC(=C2CCNCC2=N1)N1C[C@H](CC#N)N(CC1)C(=O)OCC1C=CC=CC=1)OCCOCCOCCOCCN1C(=O)C2=CC=CC=C2C1=O

InChiKey: RLYCTEGJKCAPGP-DHWXLLNHSA-N

InChi: InChI=1S/C43H54N8O9/c1-48-28-34(58-24-23-57-22-21-56-20-19-55-18-17-51-40(52)35-9-5-6-10-36(35)41(51)53)25-33(48)30-59-42-46-38-26-45-14-12-37(38)39(47-42)49-15-16-50(32(27-49)11-13-44)43(54)60-29-31-7-3-2-4-8-31/h2-10,32-34,45H,11-12,14-30H2,1H3/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:

  1. 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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