1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. SHP099

SHP099 

目录号: HY-100388 纯度: 99.80%
产品使用指南

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

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SHP099 Chemical Structure

SHP099 Chemical Structure

CAS No. : 1801747-42-1

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥620
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5 mg ¥800
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10 mg ¥1450
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50 mg ¥4800
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100 mg ¥7500
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500 mg   询价  

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 38 篇科研文献

    SHP099 purchased from MCE. Usage Cited in: Hepatology. 2018 Jul;68(1):333-348.

    Primary human HSCs are treated with SHP099 for 1 hour. PDGF-BB is added and cells are cultured for 12 additional hours. Whole cell lysates and EVs are examined by WB (n=6).

    SHP099 purchased from MCE. Usage Cited in: Nat Commun. 2019 Apr 1;10(1):1473.

    SHP099 inhibits IRS1-AP2 interaction in primary hepatocytes.

    SHP099 purchased from MCE. Usage Cited in: Open Biol. 2017 May;7(5). pii: 170066.

    Comparing the effects of SHP2 degradation and allosteric inhibition on Ras/MAPK signalling. (a) Human U2OS, A549, K-562 and MDA-MB-468 cells are treated with DMSO control or 1, 5 and 10 µM SHP099 for 2 h prior to lysis. Extracts (10 µg protein) are resolved by SDS-PAGE and transferred to nitrocellulose membranes, which are subjected to western blotting with the indicated antibodies. (b) Uninfected U2OS cells (WT) or cells infected with retroviruses encoding VHL, aCS3 and VHL-aCS3 are treated wit

    SHP099 purchased from MCE. Usage Cited in: Cancer Discov. 2018 Oct;8(10):1237-1249.

    Immunoblots of whole cell lysates or GST-RBD-precipitated (RAS-GTP, KRASGTP and NRAS-GTP) lysates from PDAC cells treated with DMSO, SHP099 10 μM, AZD6244 1 μM, or both drugs for the times indicated.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM[1].

    IC50 & Target

    IC50: 70 nM (SHP2)[1]

    体外研究
    (In Vitro)

    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[1]. 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[2].

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

    体内研究
    (In Vivo)

    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[1].

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

    分子量

    352.26

    Formula

    C16H19Cl2N5

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 12 mg/mL (34.07 mM; Need ultrasonic)

    H2O : 1 mg/mL (2.84 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.8388 mL 14.1941 mL 28.3881 mL
    5 mM 0.5678 mL 2.8388 mL 5.6776 mL
    10 mM 0.2839 mL 1.4194 mL 2.8388 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。-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: 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (28.39 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: ≥ 1.2 mg/mL (3.41 mM); Clear solution

      此方案可获得 ≥ 1.2 mg/mL (3.41 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 12.0 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
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 1.2 mg/mL (3.41 mM); Clear solution

      此方案可获得 ≥ 1.2 mg/mL (3.41 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 12.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 4.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 1.2 mg/mL (3.41 mM); Clear solution

      此方案可获得 ≥ 1.2 mg/mL (3.41 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 12.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 5.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 0.67 mg/mL (1.90 mM); Clear solution

    • 6.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.67 mg/mL (1.90 mM); Clear solution

    • 7.

      请依序添加每种溶剂: 1% DMSO    99% saline

      Solubility: ≥ 0.13 mg/mL (0.37 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    Kinase Assay
    [1]

    The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1].

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

    Cell Assay
    [1]

    Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined[1].

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

    参考文献

    纯度: 99.80%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    SHP099
    目录号:
    HY-100388
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