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)。
| 生物活性 | PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor ofFAKwith anIC50of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cellapoptosis[1]. |
体外研究
(In Vitro) | PND-1186 has an IC50of ~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].
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. |
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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].
| 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. |
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| 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 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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