PND-1186 hydrochloride - CAS:1356154-94-3

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

目录号 : KM11191 CAS No. : 1356154-94-3 纯度 : 98%

Data Sheet 产品使用指南

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)。

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500mg	询价	In-stock

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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.

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.

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

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.

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.

分子式

C₂₅H₂₇ClF₃N₅O₃

分子量

537.96

CAS号

1356154-94-3

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 : 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。-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。
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。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

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