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  • SHP-099盐酸盐

SHP-099盐酸盐

SHP099 hydrochloride
询价 5mg 起订
25mg 起订
上海 更新日期:2023-10-16

爱必信(上海)生物科技有限公司

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产品详情:

中文名称:
SHP-099盐酸盐
英文名称:
SHP099 hydrochloride
保存条件:
store at -20℃ for one year(Powder)
纯度规格:
>98 %
产品类别:
激动剂抑制剂

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抑制剂描述:

产品名称:SHP099 hydrochloride

产品别名:SHP-099盐酸盐

英文别名:SHP099 HCl

靶点:SHP2

CAS:1801747-11-4

 

纯度:>98 %

外观:粉剂

保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

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.

 

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)

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.

 

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.

 

产品信息订购:

  产品货号
  产品名称
  规格
价格
大包装及货期
  abs810051
  SHP099 hydrochloride
  5mg
  750
  立即咨询

产品更多信息请进入爱必信网站咨询

SHP-099盐酸盐; SHP099 hydrochloride

公司简介

爱必信(上海)生物科技有限公司成立于2010年,位于上海市申江科创园。是一家自主研发和生产生物试剂的公司。 Absin?是爱必信(上海)生物科技有限公司的试剂品牌,目前已近60万种生化试剂,10万种抗体,其基础生化试剂在基础科学领域得到广泛应用的同时,特色产品线常规生化试剂,血清,小分子激动剂及抑制剂在业界也备受好评。 Absin秉承踏实,务实,求精和不断创新的精神为中国科学家提供最好的产品,努力打造属于中国自己的生物试剂品牌,为广大科学家提供更全面更丰富更优质的产品。 爱科研,必信它(Absin)!Absin努力成为你身边的科研百宝箱!

成立日期 (14年)
注册资本 2500万
员工人数 100-500人
年营业额 ¥ 1000万-5000万
经营模式 工厂
主营行业 生化试剂,抗体,分子生物学,生物活性小分子

SHP-099盐酸盐相关厂家报价 更多

  • 1801747-11-4
  • 1801747-11-4
  • 河南威梯希化工科技有限公司 VIP
  • 2024-03-29
  • 询价
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