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SHP099 {[allProObj[0].p_purity_real_show]}

货号:A766981 Ambeed 开学季,买赠积分,赢豪礼

SHP099是一种高效、选择性和口服可用的SHP2抑制剂,IC50为70 nM。

SHP099 化学结构 CAS号:1801747-42-1
SHP099 化学结构
CAS号:1801747-42-1
SHP099 3D分子结构
CAS号:1801747-42-1
SHP099 化学结构 CAS号:1801747-42-1
SHP099 3D分子结构 CAS号:1801747-42-1
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SHP099 纯度/质量文件 产品仅供科研

货号:A766981 标准纯度: {[allProObj[0].p_purity_real_show]}
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SHP099 生物活性

描述 SHP099 is a highly potent and selective SHP2 inhibitor that can be administered orally, exhibiting an IC50 of 70 nM. The X-ray co-crystal structure of SHP099 bound to SHP2 unveils a novel interaction between the basic amine and the Phe113 backbone carbonyl. SHP099 demonstrates an ability to inhibit cell proliferation in the KYSE-520 model with an IC50 of 1.4 μM. Additionally, SHP099 is characterized by its high solubility and permeability, without significant efflux in Caco-2 cells[1]. SHP099 simultaneously interacts with the interfaces of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thereby allosterically inhibiting SHP2 activity. It also impedes RAS–ERK signaling, which is crucial in halting the proliferation of human cancer cells driven by receptor tyrosine kinases[2].

SHP099 动物研究

Animal study Following administration of a single dose at 30 mg/kg and 100 mg/kg, a dose-responsive relationship is evident in the exposure and modulation of the pharmacodynamic biomarker p-ERK within the xenografts. Administering a daily oral dose of 10 mg/kg or 30 mg/kg results in tumor growth inhibition of 19% and 61%, respectively. Complete tumor stasis is observed with a daily dose of 100 mg/kg[1].

SHP099 参考文献

[1]Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.

[2]Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.

SHP099 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.84mL

0.57mL

0.28mL

14.19mL

2.84mL

1.42mL

28.39mL

5.68mL

2.84mL

SHP099 技术信息

CAS号1801747-42-1
分子式C16H19Cl2N5
分子量 352.262
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 12 mg/mL(34.07 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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