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Sarm-Nutlin Protac

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SARM-nutlin PROTAC is a MDM2-based PROTAC consisting of a non-steroidal androgen receptor ligand (SARM) and a Nutlin, linked via a PEG-based linker.

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Molecular Formula

C57H61Cl2F3N8O14

Molecular Weight

1208.36

Sarm-Nutlin Protac

- Specification
  - Related CAS
    
    1096439-26-7 (rel-(+)-isomer)
    
    Shelf Life
    
    2 years
    
    IUPAC Name
    
    (2S)-3-[4-[[2-[2-[2-[2-[[2-[4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-2-oxopiperazin-1-yl]acetyl]amino]ethoxy]ethoxy]ethoxy]acetyl]amino]phenoxy]-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
    
    Synonyms
    
    (S)-3-(4-(1-(4-((4R,5S)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)-2-oxopiperazin-1-yl)-2-oxo-6,9,12-trioxa-3-azatetradecan-14-amido)phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)phenyl)propanamide; 14-(4-{[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazol-1-yl]carbonyl}-2-oxo-1-piperazinyl)-N-{4-[(2S)-2-hydroxy-2-methyl-3-{[4-nitro-3-(trifluoromethyl)phenyl]amino}-3-oxopropoxy]phenyl}-13-oxo-3,6,9-trioxa-12-azatetradecan-1-amide; 1-Piperazineacetamide, 4-[[(4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-N-[2-[2-[2-[2-[[4-[(2S)-2-hydroxy-2-methyl-3-[[4-nitro-3-(trifluoromethyl)phenyl]amino]-3-oxopropoxy]phenyl]amino]-2-oxoethoxy]ethoxy]ethoxy]ethyl]-2-oxo-
- Properties
  - Density
    
    1.40±0.1 g/cm3
    
    InChI Key
    
    VKTBFTIPDGAIPC-BIOIQHPWSA-N
    
    InChI
    
    InChI=1S/C57H61Cl2F3N8O14/c1-35(2)84-47-30-43(79-4)18-19-44(47)53-66-51(36-5-9-38(58)10-6-36)52(37-7-11-39(59)12-8-37)69(53)55(75)68-23-22-67(50(73)32-68)31-48(71)63-21-24-80-25-26-81-27-28-82-33-49(72)64-40-13-16-42(17-14-40)83-34-56(3,76)54(74)65-41-15-20-46(70(77)78)45(29-41)57(60,61)62/h5-20,29-30,35,51-52,76H,21-28,31-34H2,1-4H3,(H,63,71)(H,64,72)(H,65,74)/t51-,52+,56+/m1/s1
    
    Canonical SMILES
    
    CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCN(C(=O)C3)CC(=O)NCCOCCOCCOCC(=O)NC4=CC=C(C=C4)OCC(C)(C(=O)NC5=CC(=C(C=C5)[N+](=O)[O-])C(F)(F)F)O)C6=CC=C(C=C6)Cl)C7=CC=C(C=C7)Cl
- Reference Reading
  - 1. Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.
    
    Schneekloth, A.R., Pucheault, M., Tae, H.S. and Crews, C.M., 2008. Bioorganic & medicinal chemistry letters, 18(22), pp.5904-5908.
    
    We have developed a heterobifunctional all-small molecule PROTAC (PROteolysis TArgeting Chimera) capable of inducing proteasomal degradation of the androgen receptor. This cell permeable PROTAC consists of a non-steroidal androgen receptor ligand (SARM) and the MDM2 ligand known as nutlin, connected by a PEG-based linker. The SARM-nutlin PROTAC recruits the androgen receptor to MDM2, which functions as an E3 ubiquitin ligase. This leads to the ubiquitination of the androgen receptor, and its subsequent degradation by the proteasome. Upon treatment of HeLa cells with 10 μM PROTAC for 7 h, we were able to observe a decrease in androgen receptor levels. This degradation is proteasome dependent, as it is mitigated in cells pre-treated with 10 μM epoxomicin, a specific proteasome inhibitor. These results have implications for the potential study and treatment of various cancers with increased androgen receptor levels.

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