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SHP099

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Chemical Structure| 1801747-42-1 同义名 : -
CAS号 : 1801747-42-1
货号 : A766981
分子式 : C16H19Cl2N5
纯度 : 99%+
分子量 : 352.262
MDL号 : MFCD29059453
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：
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].
实验方案
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
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.