PND-1186|1061353-68-1|(VS-4718; SR-2516)-陌孚医药/Medlife

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

目录号: PL03812 纯度: ≥99%

CAS No. :1061353-68-1

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中文名称	PND-1186
中文别名	PND-1186 (VS-4718) 抑制剂
英文名称	PND-1186
英文别名	2-{[2-{[2-Methoxy-4-(4-morpholinyl)phenyl]amino}-5-(trifluorometh yl)-4-pyridinyl]amino}-N-methylbenzamide hydrochloride (1:1);2-(2-(2-ethoxyethoxy)ethoxy)ethyl 4-methylbenzenesulfonate;triethylene glycol monoethyl ether p-toluenesulfonate;Ethanol, 2-[2-(2-ethoxyethoxy)ethoxy]-, 4-methylbenzenesulfonate;monotosyloxy triethylene glycol monoethyl ether;CTK2B0645;triethylene glycol monoethyl ether p-tosylate;N-methyl-2-{[2-{[2-(methyloxy)-4-(4-morpholinyl)phenyl]amino}-5-(trifluoromethyl)-4-pyridinyl]amino}benzamide;2-(2-(2-methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide;2-[2-(2-ethoxyethoxy)ethoxy]ethyl 4-methylbenzenesulfonate;PND-1186;2-{[2-{[2-Methoxy-4-(4-morpholinyl)phenyl]amino}-5-(trifluorometh yl)-4-pyridinyl]amino}-N-methylbenzamide hydrochloride (1:1;PND-1186 (VS-4718);VS-4718(PND1186);SR 2516;SR-2516;triethyleneglycol monoethyl;VS 4718;VS-4718;PND 1186;2-[[2-[[2-Methoxy-4-(4-morpholinyl)phenyl]amino]-5-(trifluoromethyl)-4-pyridinyl]amino]-N-methylbenzamide;SR-2156;PND1186;L2BD0MW4OL;SR2516;2-((2-((2-Methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide;2-[[2-(2-methoxy-4-morpholin-4-ylanilino)-5-(trifluoromethyl)pyridin-4-yl]amino]-N-methylbenzamide;Benzamide, 2-[[2-[[2-methoxy-4-(4-morpholinyl)ph
Cas No.	1061353-68-1
分子式	C₂₅H₂₆F₃N₅O₃
分子量	501.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 IC 50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.

性状

Solid

IC50 & Target[1][2]

IC50: 1.5 nM (FAK)

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

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : ≥ 34 mg/mL (67.80 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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