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Autophagy-IN-2

产品编号 T60749 CAS 2755454-90-9

Autophagy-IN-2 (Compound 7h) 是自噬通量的抑制剂，可诱导癌细胞凋亡，具有研究三阴性乳腺的潜力。

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Autophagy-IN-2, CAS 2755454-90-9

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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生物活性

化学信息

存储 & 溶解度

产品描述	Autophagy-IN-2 (Compound 7h) is an inhibitor of autophagic flux which induces cancer cell apoptosis and can be used for the research of triple-negative breast cancer [1].
体外活性	Autophagy-IN-2 (Compound 7h) (0-200 μM, 48 h) shows anti-viability activities against various cancer cells [1]. Autophagy-IN-2 (0-20 μM, 0-48 h) suppresses autophagic flux and impairs DNA repair through down-regulating chromatin ubiquitination in a p62-dependent manner [1]. Autophagy-IN-2 (0-20 μM, 48 h) induces cell cycle arrest at S-phase and mitochondria-dependent intrinsic apoptosis [1]. Cell Viability Assay [1] Cell Line: MDA-MB-231, MDA-MB-468, SCC25, HSC-3, HCT116, SW620, PC3, Aspc, PNAC, U87, U251 and LN229 Concentration: 0-200 μM Incubation Time: 48 h Result: Showed anti-viability activities with IC 50 values of 8.31 ± 1.05, 6.03 ± 0.82, 18.64 ± 2.92, 24.03 ± 3.75, 35.53 ± 7.52, 25.43 ± 2.42, 17.48 ± 1.27, 26.89 ± 5.23, 19.25 ± 3.96, 15.37 ± 1.78, 12.92 ± 2.38 and 61.35 ± 11.61 μM against MDA-MB-231, MDA-MB-468, SCC25, HSC-3, HCT116, SW620, PC3, Aspc, PNAC, U87, U251 and LN229 cells, respectively. Western Blot Analysis [1] Cell Line: MDA-MB-231 and MDA-MB-468 Concentration: 5, 10 and 20 μM Incubation Time: 0, 6, 12, 24, 36 and 48 h Result: Significantly induced to LC3B-II in a dose - and time-dependent manner, resulted in a p62 accumulation in TNBC cells, increased γH2AX in a dose and time-dependent manner, activated the phosphorylation of ATM, NBS1 and SMC1, increased p62 in the nucleus and cytoplasm in a dose-dependent manner, and significantly reduced DNA-damage-induced formation of H2A poly-ubiquitin chains. Decreased the cellular levels of Cyclin A, Cyclin B, CDK1 and CDK2, increased P21 and the phosphorylation levels of CHK1 (Serine 345) and CHK2 (Threonine 68), and increased cytochrome c, cleaved caspase-3, cleaved caspase-9 and cleaved PAPR in a dose-dependent manner. Cell Cycle Analysis [1] Cell Line: MDA-MB-231 and MDA-MB-468 Concentration: 5, 10 and 20 μM Incubation Time: 48 h Result: Induced cell cycle arrest at S-phase. Apoptosis Analysis [1] Cell Line: MDA-MB-231 and MDA-MB-468 Concentration: 5, 10 and 20 μM Incubation Time: 48 h Result: Dramatically induced cell apoptosis in TNBC cells and obviously increase the proportion of late-phase apoptosis in a dose-dependent manner.
体内活性	Autophagy-IN-2 (Compound 7h) (5 and 15 mg/kg; i.p.; every 3 days for 3 weeks) suppresses tumor growth in a dose-dependent manner [1]. Animal Model: Six-week-old female NOD/SCID mice, MDA-MB-231 xenograft [1] Dosage: 5 mg/kg, 15 mg/kg Administration: Intraperitoneal injection, every 3 days for 3 weeks Result: Suppressed human TNBC tumor growth in a dose-dependent manner and resulted in a concentration-dependent upregulation of LC3B-II, p62, γH2AX and PARP.

分子量	309.37
分子式	C17H19N5O
CAS No.	2755454-90-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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稀释计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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