GW280264X

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GW280264X  纯度: 97.36%

GW280264X 是 ADAM10/TACE (ADAM17) 金属蛋白酶抑制剂。GW280264X 有效阻断 TACE (ADAM17)ADAM10IC50 分别为 8.0 nM 和 11.5 nM。ADAM10/17 可调节胶质母细胞瘤起始细胞的免疫原性。

GW280264X

GW280264X Chemical Structure

CAS No. : 866924-39-2

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10 mg ¥7500 In-stock
25 mg ¥15800 In-stock
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GW280264X 相关产品

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生物活性

GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2].

IC50 & Target[1]

ADAM17

8 nM (IC50)

ADAM10

11.5 nM (IC50)

体外研究
(In Vitro)

The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Glioblastoma-initiating cells (GIC) GS-7 cells
Concentration: 0.1, 1, and 3 µM
Incubation Time: 48 hours
Result: Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17.

体内研究
(In Vivo)

Pharmacological inhibition of ADAM10 and ADAM17 improves functional recovery after spinal cord injury (SCI)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[3]
Dosage: 100  µg/kg
Administration: I.p. injected; every day for one week starting 4 h post-surgery
Result: Showed significantly improved functional recovery compared to the control group.

分子量

575.72

Formula

C28H41N5O6S

CAS 号

866924-39-2

运输条件

Room temperature in continental US; may vary elsewhere.

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

DMSO : 125 mg/mL (217.12 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7370 mL 8.6848 mL 17.3696 mL
5 mM 0.3474 mL 1.7370 mL 3.4739 mL
10 mM 0.1737 mL 0.8685 mL 1.7370 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: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.61 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.61 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Christian Hundhausen, et al. The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion. Blood. 2003 Aug 15;102(4):1186-95.

    [2]. Fabian Wolpert, et al. A disintegrin and metalloproteinases 10 and 17 modulate the immunogenicity of glioblastoma-initiating cells. Neuro Oncol. 2014 Mar;16(3):382-91.

    [3]. Daniela Sommer, et al. ADAM17-deficiency on microglia but not on macrophages promotes phagocytosis and functional recovery after spinal cord injury. Brain Behav Immun. 2019 Aug;80:129-145.

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