2458219-65-1
Chemical Structure
SHP2-D26
- CAS No.: 2458219-65-1
- Formula:C56H79ClN12O6S2
- Molecular Weight:1115.89
IUPAC Name: (2S,4R)-1-((S)-2-(9-(4-(4-((3-((3-amino-5-(4-amino-4-methylpiperidin-1-yl)pyrazin-2-yl)thio)-2-chlorophenyl)amino)-4-oxobutanoyl)piperazin-1-yl)nonanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
InChIKey: XJSPAQRZSJUBLB-WQFCSRJTSA-N
SMILES: ClC(C(SC1=NC=C(N2CCC(N)(CC2)C)N=C1N)=CC=C3)=C3NC(CCC(N(CC4)CCN4CCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O)=O)=O
Biological Activity: SHP2-D26 is a SHP2 PROTAC degrader with DC50 values of 6.0 nM (KYSE520 cells) and 2.6 nM (MV4;11 cells), respectively. SHP2-D26 inhibits ERK phosphorylation, upregulates Bim levels, downregulates Mcl-1 levels, and induces cell cycle arrest and apoptosis. SHP2-D26 can be used in studies related to esophageal cancer, acute myeloid leukemia and non-small cell lung cancer[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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SHP2-D26 | 95.83% | SHP2-D26 is a SHP2 PROTAC degrader with DC50 values of 6.0 nM (KYSE520 cells) and 2.6 nM (MV4;11 cells), respectively. SHP2-D26 inhibits ERK phosphorylation, upregulates Bim levels, downregulates Mcl-1 levels, and induces cell cycle arrest and apoptosis. SHP2-D26 can be used in studies related to esophageal cancer, acute myeloid leukemia and non-small cell lung cancer. | ||||||||||||||||||||
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References
- [1]. Wang M, et al. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein. Journal of medicinal chemistry. 2020 Jul 23;63(14):7510-7528. [Content Brief]
- [2]. Deng Y, et al. Therapeutic efficacy of the novel SHP2 degrader SHP2-D26, alone or in combination, against lung cancer is associated with modulation of p70S6K/S6, Bim and Mcl-1. Cancer gene therapy. 2022 Nov;29(11):1558-1569. [Content Brief]
