PND-1186 VS-4718; SR-2516|cas:1061353-68-1|西域试剂

PND-1186 VS-4718; SR-2516,99.78%

产品编号：Bellancom-13917| CAS NO：1061353-68-1| 分子式：C₂₅H₂₆F₃N₅O₃| 分子量：501.50

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-13917	￥730.00	杭州北京（现货）
Bellancom-13917	￥1100.00	杭州北京（现货）
Bellancom-13917	￥1500.00	杭州北京（现货）
Bellancom-13917	￥4200.00	杭州北京（现货）
Bellancom-13917	￥7500.00	杭州北京（现货）

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PND-1186 VS-4718; SR-2516

产品介绍

PND-1186 (VS-4718) 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 选择性促进肿瘤细胞凋亡 (apoptosis)。

生物活性

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

体外研究

PND-1186 has an IC₅₀ of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397.
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.

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

Western Blot Analysis

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.

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

Animal Model:	BALB/c mice
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.

体内研究

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.

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

Animal Model:	BALB/c mice
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.

体内研究

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.

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

Animal Model:	BALB/c mice
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 34 mg/mL (67.80 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	1.9940 mL	9.9701 mL	19.9402 mL
5 mM	0.3988 mL	1.9940 mL	3.9880 mL
10 mM	0.1994 mL	0.9970 mL	1.9940 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 (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 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: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution