SHP2-IN-23

• 常用名: SHP2-IN-23
• 英文名: SHP2-IN-23
• CAS号: 2415989-91-0
• 分子量: 491.01
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₃ClN₈S
• 熔点: N/A
• 闪点: N/A

SHP2-IN-23用途

SHP2-IN-23 (compound 30) 是一种口服有效的 SHP2 抑制剂 (IC50=38 nM),优异的体内功效和药代动力学特征。SHP2-IN-23 抑制 ERK 磷酸化,IC50=5 nM。

SHP2-IN-23名称

• 英文名: SHP2-IN-23

SHP2-IN-23生物活性

• 描述: SHP2-IN-23 (compound 30) 是一种口服有效的 SHP2 抑制剂 (IC50=38 nM),优异的体内功效和药代动力学特征。SHP2-IN-23 抑制 ERK 磷酸化,IC50=5 nM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> MAPK/ERK信号通路 >> ERK
  信号通路 >> 干细胞及 Wnt 通路 >> ERK
• 靶点实验:

  IC50: 38 nM (SHP2), 5 nM (pERK)[1]

• 参考文献:

  [1]. Elsayed M S A et al. Discovery of 5-Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors[J]. ACS Medicinal Chemistry Letters, 2023.

SHP2-IN-23物理化学性质

• 分子式: C₂₄H₂₃ClN₈S
• 分子量: 491.01

SHP2-IN-23靶点实验

查看更多实验

实验名称：Inhibition of ERK1/2 phosphorylation at Thr202/Tyr204 residues in human KYSE520 cells... 来源：ChEMBL 靶标：Mitogen-activated protein kinase 3 External Id：CHEMBL5393395

实验名称：Allosteric inhibition of recombinant full length 6His-tagged SHP2 (2 to 527 residues)... 来源：ChEMBL 靶标：Tyrosine-protein phosphatase non-receptor type 11 External Id：CHEMBL5393394

实验名称：Inhibition of ERK1/2 phosphorylation at Thr202/Tyr204 residues in human KYSE520 cells... 来源：ChEMBL 靶标：Mitogen-activated protein kinase 3 External Id：CHEMBL5393416

实验名称：Antitumor activity against human MIA PaCa-2 cells harboring KRAS G12C mutant xenograf... 来源：ChEMBL 靶标：MIA PaCa-2 External Id：CHEMBL5393415

实验名称：Antitumor activity against human MIA PaCa-2 cells harboring KRAS G12C mutant xenograf... 来源：ChEMBL 靶标：MIA PaCa-2 External Id：CHEMBL5393414

实验名称：Toxicity in athymic nude Foxn1nu mouse xenografted with human MIA PaCa-2 cells harbor... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5393413

实验名称：In vivo inhibition of SHP2 in po dosed athymic nude Foxn1nu mouse xenografted with hu... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5393412

实验名称：AUC(0 to infinity) in CD-1 mouse at 10 mg/kg, po measured upto 24 hrs by LC-MS/MS met... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5393411

实验名称：Oral bioavailability in CD-1 mouse at 10 mg/kg measured upto 24 hrs by LC-MS/MS metho... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5393410

实验名称：Tmax in CD-1 mouse at 10 mg/kg, po measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5393408

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