CRBN PROTAC 14a, CAS No. 2358775-70-7, is a cereblon degrader. It comprises a ligand for Von Hippel Lindau (VHL) protein joined by a linker to a cereblon targeting ligand. It preferentially degrades cereblon, and induces rapid and profound cereblon degradation.

Product information

CAS Number: 2358775-70-7

Molecular Weight: 1061.25

Formula: C53H72N8O13S

Synonym:

CRBN PROTAC 14a

CRBN-PROTAC-14a

CRBN PROTAC14a

Chemical Name: N1-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-N20-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,9,12,18-tetraoxaicosanediamide

Smiles: CC1N=CSC=1C1C=CC(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCCCCOCCOCCCCCOCC(=O)NCCNC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)=CC=1

InChiKey: PEZCAXDTKNFUCR-CTMFSBKBSA-N

InChi: InChI=1S/C53H72N8O13S/c1-34-46(75-33-57-34)36-16-14-35(15-17-36)29-56-48(66)41-28-37(62)30-60(41)52(70)47(53(2,3)4)58-44(65)32-74-25-10-6-8-23-72-27-26-71-22-7-5-9-24-73-31-43(64)55-21-20-54-39-13-11-12-38-45(39)51(69)61(50(38)68)40-18-19-42(63)59-49(40)67/h11-17,33,37,40-41,47,54,62H,5-10,18-32H2,1-4H3,(H,55,64)(H,56,66)(H,58,65)(H,59,63,67)/t37-,40?,41+,47-/m1/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

References:

1. Girardini M, Maniaci C, Hughes SJ, Testa A, Ciulli A. Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorg Med Chem. 2019 Jun 15;27(12):2466-2479. doi: 10.1016/j.bmc.2019.02.048. Epub 2019 Feb 22. PMID: 30826187; PMCID: PMC6561380.

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