货号	规格	价格	上海	北京	武汉	南京
S80478-1mg	99.80%	￥275.00 S80478-1mg ￥275.00 现货	4 4	-	-	-
S80478-5mg	99.80%	￥600.00 S80478-5mg ￥600.00 现货	8 8	-	-	-
S80478-10mg	99.80%	￥980.00 S80478-10mg ￥980.00 现货	4 4	-	-	-
S80478-25mg	99.80%	￥1770.00 S80478-25mg ￥1770.00 现货	5 5	-	-	-
S80478-50mg	99.80%	￥2680.00 S80478-50mg ￥2680.00 现货	2 2	-	-	-
S80478-100mg	≥98%	￥3750.00 S80478-100mg ￥3750.00 2-3天	0 货期：2-3天	-	-	-

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产品描述：

SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM

靶点：

IC50: 70 nM (SHP2);Phosphatase;PERK

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

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.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.839 ml	14.194 ml	28.388 ml
5 mM	0.568 ml	2.839 ml	5.678 ml
10 mM	0.284 ml	1.419 ml	2.839 ml
50 mM	0.057 ml	0.284 ml	0.568 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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