PND-1186 hydrochloride(Synonyms: VS-4718 hydrochloride; SR-2516 hydrochloride)

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PND-1186 hydrochloride (Synonyms: VS-4718 hydrochloride; SR-2516 hydrochloride) 纯度: 98.78%

PND-1186 hydrochloride (VS-4718 hydrochloride) 是一种有效的，高特异性的，可逆的 FAK 抑制剂，IC50 为 1.5 nM。PND-1186 hydrochloride 选择性促进肿瘤细胞凋亡 (apoptosis)。

PND-1186 hydrochloride(Synonyms: VS-4718 hydrochloride; SR-2516 hydrochloride)

PND-1186 hydrochloride Chemical Structure

CAS No. : 1356154-94-3

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 ￥1302 In-stock
5 mg ￥1100 In-stock
10 mg ￥1500 In-stock
50 mg ￥4200 In-stock
100 mg ￥7500 In-stock
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500 mg   询价  

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PND-1186 hydrochloride 相关产品

•相关化合物库:

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生物活性

PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis[1].

体外研究
(In Vitro)

PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397[1].
In murine 4T1 breast carcinoma cells, FAK is important in promoting an invasive and metastatic cell phenotype. Increasing concentrations of PND-1186 (0.1 to 1.0 µM) added to 4T1 cells inhibits FAK Tyr-397 phosphorylation (pY397) and results in elevated levels of total FAK protein within 1 h[1].

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.

Western Blot Analysis[1]

Cell Line: 4T1 breast carcinoma cells
Concentration: 0.1, 0.2, 0.4, 0.6 and 1.0 µM
Incubation Time: 1 hour
Result: Inhibited FAK Tyr-397 phosphorylation (pY397) and resulted in elevated levels of total FAK protein.

体内研究
(In Vivo)

PND-1186 (30 mg/kg or 100 mg/kg; subcutaneously; injected subcutaneously in the neck region) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis[1].

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: BALB/c mice[1]
Dosage: 30 mg/kg or 100 mg/kg
Administration: Injected (100 µL) subcutaneously in the neck region; every 12 h (twice-daily, b.i.d.) for 5 days.
Result: 100 mg/kg treatment significantly reduced final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly reduced final tumor weight but was not significantly different compared to control.

Clinical Trial

分子量

537.96

Formula

C25H27ClF3N5O3
CAS 号

1356154-94-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (371.77 mM; Need ultrasonic)

H2O : 20 mg/mL (37.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8589 mL 9.2944 mL 18.5887 mL
5 mM 0.3718 mL 1.8589 mL 3.7177 mL
10 mM 0.1859 mL 0.9294 mL 1.8589 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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (9.29 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (9.29 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (9.29 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (9.29 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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
*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]. Tanjoni I, et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.

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