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SHP-099盐酸盐;1801747-11-4

简要描述:SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models.

  • 产品型号:abs810051
  • 厂商性质:生产厂家
  • 更新时间:2024-07-07
  • 访  问  量:1402

详细介绍

品牌absinCAS1801747-11-4
分子式C16H20Cl3N5纯度>98 %
分子量388.72货号abs810051
规格5mg;25mg;100mg供货周期现货
主要用途-应用领域化工,生物产业,综合
产品描述
描述

SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP-099 stabilizes SHP2 in an auto-inhibited conformation, concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro and is efficacious in mouse tumor xenograft models. SHP099’s activity provides evidence that pharmacological inhibition of SHP2 is a viable strategy to target RTK-driven cancers and presents a new chemical tool for further interrogation of the multifaceted cellular functions of SHP2 in development, tumorigenesis, RTK-driven drug resistance and immune-checkpoint modulation.SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest.

纯度>98 %
储存/保存方法Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名SHP-099盐酸盐;SHP099 HCl
外观粉剂
可溶性/溶解性Water : 7.69 mg/mL(19.78 mM), Need ultrasonic and warming

DMSO : 4.1 mg/mL (10.55 mM; Need ultrasonic and warming)
生物活性
靶点SHP2
In vitro(体外研究)The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC50 of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells.
In vivo(体内研究)After a single doses of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg.
分子结构图

温馨提示:本产品仅作科研实验使用,不支持临床等研究

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