2458219-65-1
中文名称
(2S,4R)-1-((S)-2-(9-(4-(4-((3-((3-氨基-5-(4-氨基-4-甲基哌啶-1-基)吡嗪-2-基)硫基)-2-氯苯基)氨基)-4-氧代丁酰基)哌嗪-1-基)壬酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-((S)-1-(4-(4-甲基噻唑-5-基)苯基)乙基)吡咯烷-2-甲酰胺
英文名称
INDEX NAME NOT YET ASSIGNED
CAS
2458219-65-1
分子式
C56H79ClN12O6S2
分子量
1115.9
MOL 文件
2458219-65-1.mol
更新日期
2024/07/24 18:26:20
2458219-65-1 结构式
基本信息
中文别名
(2S,4R)-1-((S)-2-(9-(4-(4-((3-((3-氨基-5-(4-氨基-4-甲基哌啶-1-基)吡嗪-2-基)硫基)-2-氯苯基)氨基)-4-氧代丁酰基)哌嗪-1-基)壬酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-((S)-1-(4-(4-甲基噻唑-5-基)苯基)乙基)吡咯烷-2-甲酰胺 英文别名
SHP2-D26物理化学性质
沸点1240.1±65.0 °C(Predicted)
密度1.33±0.1 g/cm3(Predicted)
酸度系数(pKa)13.10±0.70(Predicted)
形态Solid
颜色Off-white to light yellow
应用领域
用途一
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.