货号	规格	价格	上海	北京	珠海	重庆	武汉
S84019-1mg买3赠1	99.85%	￥140.00 S84019-1mg ￥140.00 现货（买3赠1）	1003 >10	-	-	-	-
S84019-5mg买3赠1	99.85%	￥190.00 S84019-5mg ￥190.00 现货（买3赠1）	203 >10	-	-	-	-
S84019-10mg买3赠1	99.85%	￥255.00 S84019-10mg ￥255.00 现货（买3赠1）	107 >10	-	-	-	-
S84019-25mg买3赠1	99.85%	￥345.00 S84019-25mg ￥345.00 现货（买3赠1）	45 >10	-	-	-	-
S84019-50mg买3赠1	99.85%	￥460.00 S84019-50mg ￥460.00 现货（买3赠1）	25 >10	-	-	-	-
S84019-100mg	99.85%	￥610.00 S84019-100mg ￥610.00 现货	13 >10	-	-	-	-

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产品描述：

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

靶点：

IC50: 70 nM (SHP2)

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. 3. Carmine Fedele, et al. SHP2 Inhibition Abrogates MEK inhibitor Resistance in Multiple Cancer Models. bioRxiv. April 25, 2018.

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	2.573 ml	12.863 ml	25.725 ml
5 mM	0.515 ml	2.573 ml	5.145 ml
10 mM	0.257 ml	1.286 ml	2.573 ml
50 mM	0.051 ml	0.257 ml	0.515 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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