Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Amsilarotene (TAC101) 是口服有活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡,可用于研究癌症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 595 | 现货 | ||
5 mg | ¥ 1,470 | 现货 | ||
10 mg | ¥ 2,390 | 现货 | ||
25 mg | ¥ 3,970 | 现货 | ||
50 mg | ¥ 5,780 | 现货 | ||
100 mg | ¥ 7,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,630 | 现货 |
产品描述 | Amsilarotene (TAC101) inhibits the phosphorylation of retinoblastoma gene product (RB) and increases the presence of 2 cyclin-dependent kinases (CDK) inhibitors resulting in cell cycle arrest. This agent also causes a cytotoxic decline in the thymidylate synthase and cyclin A expression. |
靶点活性 | RARβ:400 nM (Ki), RARα:2.4 nM (Ki) |
体外活性 | Preclinical models have shown that Amsilarotene(4-[3,5-bis(trimethylsilyl) benzamide] benzoic acid), an oral synthetic retinoid, has antitumor activity in hepatocellular carcinoma (HCC). |
体内活性 | We conducted a phase I study in Japanese patients with advanced HCC to examine the pharmacokinetics, recommended dose, safety, and efficacy of Amsilarotene. The administered dose of Amsilarotene was 10 mg/day in four patients (level 1), 20 mg/day in six (level 2), and 30 mg/day in three (level 3). There was no dose-limiting toxicity at level 1. Only one patient each had dose-limiting toxicity at level 2 (grade 2 fatigue, recovery requiring eight or more consecutive days of rest) and at level 3 (grade 3 splenic vein thrombosis). Level 3 (30 mg/day) was considered the maximum tolerated dose and 20 mg/day the recommended dose by a panel of medical experts, placing maximum emphasis on safety. The most frequent adverse events were fatigue, headache, and dermal symptoms such as rash. Pharmacokinetic parameters in Japanese patients with HCC were similar to those in patients in the United States, most of whom were Caucasian. Although no patient had a complete or partial response, the disease control rate was 38.5%. In conclusion, the recommended dose of Amsilarotene for patients with HCC is 20 mg/day. Amsilarotene had an acceptable toxicity profile, warranting further evaluation in clinical trials. |
别名 | TAC-101, TAC 101, TAC101 |
分子量 | 385.6 |
分子式 | C20H27NO3Si2 |
CAS No. | 125973-56-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/ml (155.6 mM)
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5934 mL | 12.9668 mL | 25.9336 mL | 64.834 mL |
5 mM | 0.5187 mL | 2.5934 mL | 5.1867 mL | 12.9668 mL | |
10 mM | 0.2593 mL | 1.2967 mL | 2.5934 mL | 6.4834 mL | |
20 mM | 0.1297 mL | 0.6483 mL | 1.2967 mL | 3.2417 mL | |
50 mM | 0.0519 mL | 0.2593 mL | 0.5187 mL | 1.2967 mL | |
100 mM | 0.0259 mL | 0.1297 mL | 0.2593 mL | 0.6483 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Amsilarotene 125973-56-0 Cell Cycle/Checkpoint CDK AsPC-1 Apoptosis TAC-101 orally active Retinoid X receptors cancer Inhibitor RAR/RXR TAC 101 inhibit RMG-II MIAPaCa-2 BxPC-3 Am 555S Retinoic acid receptors TAC101 inhibitor