ChemicalBook--->CAS DataBase List--->2458219-65-1

2458219-65-1

2458219-65-1 Structure

2458219-65-1 Structure
IdentificationBack Directory
[Name]

INDEX NAME NOT YET ASSIGNED
[CAS]

2458219-65-1
[Synonyms]

SHP2-D26
[Molecular Formula]

C56H79ClN12O6S2
[MOL File]

2458219-65-1.mol
[Molecular Weight]

1115.9
Chemical PropertiesBack Directory
[Boiling point ]

1240.1±65.0 °C(Predicted)
[density ]

1.33±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

13.10±0.70(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Description]

SHP2-D26 is a first, potent, and effective PROTAC degrader of SHP2 protein. 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.
[Uses]

SHP2-D26 is a first, potent and effective SHP2 degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent[1].
[References]

[1] Wang M, et al. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein [published correction appears in J Med Chem. 2021 Jan 14;64(1):906-908]. J Med Chem. 2020;63(14):7510-7528. DOI:10.1021/acs.jmedchem.0c00471
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