计算溶液所需的质量、体积或浓度。
1A-116
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
In Vitro
1A-116 (48 h) inhibits F3II and MDA-MB-231 cells proliferation in a concentration-dependent manner with IC 50 s of 4 μM and 21 μM, respectively. ?\n1A-116 (1, 10 μM; 12 h) dramatically impaires Rac1 activation, and reduces Rac1-GTP intracellular levels in a concentration-dependent manner in F3II cells. ?\n1A-116 (50, 100 μM; 12 h) blocks Rac1-P-Rex1 interaction. ?\n1A-116 (20 μM; 5 h intervals over 25 h) inhibits LN229 cells proliferation in a circadian manner. ?\n1A-116 (10 μM; 16 h) significantly reduces cell migration at 10 HPS which exhibits temporal dependence. (HPS: After the serum shock, the elapsed time (in hours) is recorded as the hours post-synchronization (HPS)). ?\n1A-116 (20, 50 μM; 6 h) induces cells apoptosis and in a circadian-dependent manner. ?\n1A-116 (100 nM) decreases the thickness of the epidermal layers of Vav2 and Rac1-mediated hyperplasia, but not the PAK1-mediated one, which exhibits the activity of inhibiting Rac1 at the GEF-Rac1 level. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 AssayCell 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 AssayCell Line: LN229 cells Concentration: 10 µM Incubation Time: 16 h Result: Reduced cell migration at 10 HPS which exhibited temporal dependence. Apoptosis AnalysisCell Line: LN229 cells Concentration: 20, 50 µM Incubation Time: 6 h Result: Induced cells apoptosis and in a circadian-dependent manner. Western Blot AnalysisCell 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.
In Vivo
1A-116 (3 mg/kg; i.v.; once a day for 21 days) demonstrates a high antimetastatic activity with about 60% formation reduction of total metastatic lung colonies in vivo and shows no apparent toxicity . ?\n1A-116 (20 mg/kg; i.p.; once a day, 73 days for ZT12, 68 days for ZT3) increases survival time when treated at ZT12 compare to ZT3 in tumor-bearing mice. (ZT: Zeitgeber time 12 (ZT12) defined as the time of lights off (local time 7 p.m.) and ZT0 defined as lights on (local time 7 a.m.)). ?\n1A-116 shows good oral availability. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:IC50: 4 µM (F3II),21 µM (MDA-MB-231),Rac1, Apoptosis
规格
规格或纯度
Moligand™,10mM in DMSO
英文名称
1A-116
生化机理
1A-116 是一种强效 Rac1 抑制剂，对 W56 残基具有特异性，能阻止 EGF 诱导的 Rac1 激活并阻断 Rac1-P-Rex1 相互作用。1A-116 可诱导细胞凋亡，并抑制细胞增殖、迁移和周期进展，其作用机制与浓度相关。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
820-285-2
分子类型
小分子
Isomeric SMILES
CC1=CC(=CC(=C1)NC(=NC2=CC=CC=C2C(F)(F)F)N)C
PubChem CID
分子量
307.31
技术文档
高级数据
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P302+P352: 如皮肤沾染：用水充分清洗。
P321: 特殊处理（请参阅此标签上的...）。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P271: 仅在室外或通风良好的地方使用。
P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。
P403+P233: 存放在通风良好的地方。保持容器密闭。
P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。
P319: 如果你感到不适，请寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
「Moligand?」是什么？
「Moligand?」是阿拉丁科学的高端产品线之一，专为多个工作流程中的高纯度应用而设计。与同类工作流程中的标准级别相比，「Moligand?」产品通常具有更严格的规格、更严谨的 QC 以及更强的批间一致性。
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1430208-73-3，分子式为 C16H16F3N3，分子量为 307.31 g/mol。
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每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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