L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)-

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L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- Suppliers list
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L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- Basic information
Product Name:L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)-
Synonyms:SHP2-D26;(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;(2S,4R)-1-[(2S)-2-[9-(4-{3-[(3-{[3-amino-5-(4-amino-4-methylpiperidin-1-yl)pyrazin-2-yl]sulfanyl}-2-chlorophenyl)carbamoyl]propanoyl}piperazin-1-yl)nonanamido]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide;Venadaparib Impurity 92;(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?, SHP2-D26;L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)-;PROTAC SHP2 degrader-1
CAS:2458219-65-1
MF:C56H79ClN12O6S2
MW:1115.89
EINECS:
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Mol File:2458219-65-1.mol
L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- Structure
L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- Chemical Properties
Boiling point 1240.1±65.0 °C(Predicted)
density 1.33±0.1 g/cm3(Predicted)
pka13.10±0.70(Predicted)
form Solid
color Off-white to light yellow
Safety Information
MSDS Information
L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- Usage And Synthesis
DescriptionSHP2-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.
UsesSHP2-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
L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- Preparation Products And Raw materials
Tag:L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)-(2458219-65-1) Related Product Information
L-Prolinamide, N-[9-[4-[4-[[3-[[3-amino-5-(4,4-dimethyl-1-piperidinyl)-2-pyrazinyl]thio]-2-chlorophenyl]amino]-1,4-dioxobutyl]-1-piperazinyl]-1-oxononyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)- SHP2 protein degrader-2 dTAGV-1 ARV-766 CC-94676 ACP5 Protein, Mouse (HEK293, His)