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目錄:愛(ài)必信(上海)生物科技有限公司>>生化試劑>>小分子化合物>> abs810051SHP-099鹽酸鹽;1801747-11-4

SHP-099鹽酸鹽;1801747-11-4
  • SHP-099鹽酸鹽;1801747-11-4
參考價(jià) 248
訂貨量 ≥1
具體成交價(jià)以合同協(xié)議為準(zhǔn)
248
≥1
具體成交價(jià)以合同協(xié)議為準(zhǔn)
  • 品牌 absin
  • 型號(hào) abs810051
  • 廠(chǎng)商性質(zhì) 生產(chǎn)商
  • 所在地 上海市
屬性

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更新時(shí)間:2024-07-07 13:31:06瀏覽次數(shù):1558評(píng)價(jià)

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CAS 1801747-11-4 純度 >98 %
分子量 388.72 分子式 C16H20Cl3N5
供貨周期 現(xiàn)貨 規(guī)格 5mg;25mg;100mg
貨號(hào) abs810051 應(yīng)用領(lǐng)域 化工,生物產(chǎn)業(yè),綜合
主要用途 -
SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models.
產(chǎn)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.

純度>98 %
儲(chǔ)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
別名SHP-099鹽酸鹽;SHP099 HCl
外觀(guān)粉劑
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
靶點(diǎn)SHP2
In vitro(體外研究)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(體內(nèi)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.
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