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SHP2-D26 - CAS 2458219-65-1

Inquiry

SHP2-D26 is a potent and effective PROTAC degrader of SHP2 protein. SHP2-D26 is >30-times more potent in inhibition of phosphorylation of extracellular signal-regulated kinase (ERK) and of cell growth than SHP099, a potent SHP2 inhibitor, in KYSE520 and MV4;11 cancer cell lines.

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Molecular Formula

C56H79ClN12O6S2

Molecular Weight

1115.89

SHP2-D26

- Specification
  - Purity
    
    >98%
    
    Solubility
    
    Soluble in DMSO
    
    Appearance
    
    Solid Powder
    
    Storage
    
    Store at -20°C
    
    IUPAC Name
    
    (2S,4R)-1-[(2S)-2-[9-[4-[4-[3-[3-amino-5-(4-amino-4-methylpiperidin-1-yl)pyrazin-2-yl]sulfanyl-2-chloroanilino]-4-oxobutanoyl]piperazin-1-yl]nonanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
    
    Synonyms
    
    (2S,4R)-1-((S)-2-(10-(4-(4-((3-((3-Amino-5-(4-amino-4-methylpiperidin-1-yl)pyrazin-2-yl)thio)-2-chlorophenyl)amino)-4-oxobutanoyl)piperazin-1-yl)decanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide; SHP2-D 26; PROTAC SHP2 degrader-1
- Properties
  - Boiling Point
    
    1240.1±65.0°C at 760 Torr
    
    Density
    
    1.33±0.1 g/cm3
    
    InChI Key
    
    XJSPAQRZSJUBLB-WQFCSRJTSA-N
    
    InChI
    
    InChI=1S/C56H79ClN12O6S2/c1-36(38-17-19-39(20-18-38)49-37(2)61-35-76-49)62-52(74)42-32-40(70)34-69(42)54(75)50(55(3,4)5)65-45(71)16-11-9-7-8-10-12-25-66-28-30-68(31-29-66)47(73)22-21-46(72)63-41-14-13-15-43(48(41)57)77-53-51(58)64-44(33-60-53)67-26-23-56(6,59)24-27-67/h13-15,17-20,33,35-36,40,42,50,70H,7-12,16,21-32,34,59H2,1-6H3,(H2,58,64)(H,62,74)(H,63,72)(H,65,71)/t36-,40+,42-,50+/m0/s1
    
    Canonical SMILES
    
    CC1=C(SC=N1)C2=CC=C(C=C2)C(C)NC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCCCCCCCN4CCN(CC4)C(=O)CCC(=O)NC5=C(C(=CC=C5)SC6=NC=C(N=C6N)N7CCC(CC7)(C)N)Cl)O
- Reference Reading
  - 1. Discovery of SHP2-D26 as a first, potent, and effective PROTAC degrader of SHP2 protein.
    
    Wang, M., Lu, J., Wang, M., Yang, C.Y. and Wang, S., 2020. Journal of medicinal chemistry, 63(14), pp.7510-7528.
    
    Src homology 2 domain-containing phosphatase 2 (SHP2) is an attractive therapeutic target for human cancers and other human diseases. Herein, we report our discovery of potent small-molecule SHP2 degraders whose design is based upon the proteolysis-targeting chimera (PROTAC) concept. This work has led to the discovery of potent and effective SHP2 degraders, exemplified by SHP2-D26. SHP2-D26 achieves DC50 values of 6.0 and 2.6 nM in esophageal cancer KYSE520 and acute myeloid leukemia MV4;11 cells, respectively, and is capable of reducing SHP2 protein levels by >95% in cancer cells. SHP2-D26 is >30-times more potent in inhibition of phosphorylation of extracellular signal-regulated kinase (ERK) and of cell growth than SHP099, a potent SHP2 inhibitor, in KYSE520 and MV4;11 cancer cell lines. This study demonstrates that induced SHP2 degradation is a very effective approach to inhibit the function of SHP2. Further optimization of these SHP2 degraders may lead to the development of a new class of therapies for cancers and other human diseases.

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