PD173955

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PD173955  纯度: 99.12%

PD173955是Src激酶家族选择性抑制剂,对Src、Yes和Abl激酶IC50值约为22nM,对FGFR_alpha_抑制性弱,对InsR和PKC无活性。

PD173955

PD173955 Chemical Structure

CAS No. : 260415-63-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1597 In-stock
5 mg ¥1452 In-stock
10 mg ¥2280 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PD173955 相关产品

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生物活性

PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC. IC50 value: 22 nM Target: Src kinase inhibitor in vitro: PD173955 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with IC50s of 500 nM and 1 μM, respectively, with an accumulation of suspended cells. Cells treated with PD173955 show a near complete redistribution to the G2-M phase of the cell cycle in comparison with control cells, and quantitation of mitotic indices by immunofluorescence microscopy shows an accompanying accumulation of mitotic cells.PD173955 shows antimitotic activity in breast cancer cells with high or low src and yes kinase activities, the antimitotic activity of PD173955 is independent of cell type or malignant transformation [1]. PD173955 inhibits both the active and inactive forms of Abl. By contrast, Imatinib only inhibits the active form of the enzyme. In addition, the Ki for inhibition of Abl by PD173955 is very low, making it a more potent inhibitor of Abl and a more effective inhibitor of cancer cell proliferation than Imatinib [2]. PD173955, a Src family-specific tyrosine kinase inhibitor, increases the susceptibility of HT29 cells to anoikis in a dose- and time-dependent manner [3].

分子量

443.35

Formula

C21H16Cl2N4OS

CAS 号

260415-63-2

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 : 10 mg/mL (22.56 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2556 mL 11.2778 mL 22.5555 mL
5 mM 0.4511 mL 2.2556 mL 4.5111 mL
10 mM 0.2256 mL 1.1278 mL 2.2556 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.64 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

  • 2.

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

    Solubility: ≥ 1 mg/mL (2.26 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.26 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 10.0 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]. Moasser MM, et al. Inhibition of Src kinases by a selective tyrosine kinase inhibitor causes mitotic arrest. Cancer Res. 1999 Dec 15;59(24):6145-52.

    [2]. Kraus GA, et al. New effective inhibitors of the Abelson kinase. Bioorg Med Chem. 2010 Sep 1;18(17):6316-21.

    [3]. Windham TC, et al. Src activation regulates anoikis in human colon tumor cell lines. Oncogene. 2002 Nov 7;21(51):7797-807.

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