| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
Y68579-5mg买3赠1 |
99.40% | ￥600.00 |
6 | - | - | - | - |
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Y68579-10mg买3赠1 |
99.40% | ￥940.00 |
6 | - | - | - | - |
|
Y68579-25mg促销 |
99.40% | ￥1600.00 ￥1280.00 |
3 | - | - | - | - |
|
Y68579-100mg促销 |
≥98% | ￥3900.00 ￥3120.00 |
货期：2-3天 | - | - | - | - |
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| 产品描述： | 1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo | ||||||||||||||||||||
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| 靶点： | IC50: 4 µM (F3II); 21 µM (MDA-MB-231). Rac1 Apoptosis;Rho | ||||||||||||||||||||
| 体外研究： | 1A-116 (48 h) 以浓度依赖性方式抑制 F3II 和 MDA-MB-231 细胞增殖，IC50 分别为 4 μM 和 21 μM。 1A-116 (1，10 μM；12 h) 在 F3II 细胞中显著削弱 Rac1 激活，并以浓度依赖性方式降低 Rac1-GTP 胞内水平。 1A-116 (50、100 μM；12 小时) 阻断 Rac1-P-Rex1 相互作用。 1A-116 (20 μM；5 小时间隔超过25 h) 以昼夜节律方式抑制 LN229 细胞增殖。1A-116 (10 μM；16 h) 在 10 HPS 时显著减少细胞迁移，表现出时间依赖性。(HPS：血清休克后，经过的时间 (小时) 记录为同步后小时数 (HPS))。 1A-116 (20、50 μM；6 h) 以昼夜节律依赖的方式诱导细胞凋亡。 1A-116 (100 nM) 减少 Vav2 和 Rac1 介导的增生的表皮层厚度，但不是 PAK1 介导的，它在 GEF-Rac1 水平上表现出抑制 Rac1 的活性。 Cell Proliferation Assay Cell Line: MDA-MB-231, F3II, LN229 cells Concentration: 20 µM Incubation Time: 48 h; 5 h intervals over 25 h. Result: Inhibited cell proliferation in a concentration-dependent and circadian manner. Cell Viability Assay Cell Line: Ker-CT human keratinocytes cells with oncogenic Vav2/Rac1 F28L/PAK1 Tyrosine 423 Concentration: 100 nM Incubation Time: Result: Inhibited Rac1 activity at the GEF-Rac1 level. Cell Migration Assay Cell Line: LN229 cells Concentration: 10 µM Incubation Time: 16 h Result: Reduced cell migration at 10 HPS which exhibited temporal dependence. Apoptosis Analysis Cell Line: LN229 cells Concentration: 20, 50 µM Incubation Time: 6 h Result: Induced cells apoptosis and in a circadian-dependent manner. Western Blot Analysis Cell Line: F3II cells Concentration: 1, 10 µM Incubation Time: 12 h Result: Blocked Rac1-P-Rex1 interaction.Reduced Rac1-GTP intracellular levels in a concentration-dependent manner. | ||||||||||||||||||||
| 体内研究： | 1A-116 (3 mg/kg；静脉注射；每天一次，持续 21 天) 显示出高抗转移活性，体内总转移性肺集落的形成减少了约 60%，并且没有表现出明显的毒性。 1A-116 (20 mg/kg；腹腔注射；每天一次，ZT12 为 73 天，ZT3 为 68 天) 与 ZT3 相比，在荷瘤小鼠中接受 ZT12 处理可延长存活时间。(ZT：Zeitgeber 时间 12 (ZT12) 定义为关灯时间 (当地时间晚上 7 点)，ZT0 定义为开灯时间 (当地时间早上 7 点))。 1A-116 显示出良好的口服可用性。 Animal Model: Female BALB/c inbred mice (8 to 10-week-old; average 20 g) Dosage: 3 mg/kg Administration: Intravenous injection; once a day for 21 days. Result: Demonstrated a high antimetastatic activity. Animal Model: Male NIH Swiss foxN1(∆/∆) nude mice (2-month-old; GBM model). Dosage: 20 mg/kg Administration: Intraperitoneal injection (at ZT3, ZT12); once a day, 73 days for ZT12, 68 days for ZT3. Result: Increased survival time when treated at ZT12 compared to ZT3 in tumor-bearing mice. | ||||||||||||||||||||
| 参考文献： | 1. Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840-51. 2. Trebucq LL, et al. Timing of Novel Drug 1A-116 to Circadian Rhythms Improves Therapeutic Effects against Glioblastoma. Pharmaceutics. 2021 Jul 16;13(7):1091. 3. González N, et al. Computational and in vitro Pharmacodynamics Characterization of 1A-116 Rac1 Inhibitor: Relevance of Trp56 in Its Biological Activity. Front Cell Dev Biol. 2020 Apr 15;8:240. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | RT | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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