SHP099 hydrochloride|cas:2200214-93-1|西域试剂

SHP099 hydrochloride,99.87%

产品编号：Bellancom-100388A| CAS NO：2200214-93-1| 分子式：C₁₆H₂₀Cl₃N₅| 分子量：388.72

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100388A	￥790.00	杭州北京（现货）
Bellancom-100388A	￥1200.00	杭州北京（现货）
Bellancom-100388A	￥2880.00	杭州北京（现货）
Bellancom-100388A	￥5280.00	杭州北京（现货）

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SHP099 hydrochloride

产品介绍

SHP099 hydrochloride是有效，选择性，有口服活性的 SHP2 抑制剂，IC₅₀值为70 nM。

生物活性

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

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 4.1 mg/mL (10.55 mM; Need ultrasonic and warming)

H₂O : ≥ 2.5 mg/mL (6.43 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5725 mL	12.8627 mL	25.7255 mL
5 mM	0.5145 mL	2.5725 mL	5.1451 mL
10 mM	0.2573 mL	1.2863 mL	2.5725 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 50% PEG300 50% saline
Solubility: 20 mg/mL (51.45 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液