Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TASIN-1 是截短的APC 基因(结肠腺瘤样息肉基因)选择性抑制剂,可以抑制胆固醇生物合成并发挥细胞毒性作用。它是一种预防和干预APC 突变型结直肠癌的潜在治疗策略。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 329 | 现货 | ||
5 mg | ¥ 778 | 现货 | ||
10 mg | ¥ 1,370 | 现货 | ||
25 mg | ¥ 2,830 | 现货 | ||
50 mg | ¥ 4,220 | 现货 | ||
100 mg | ¥ 5,890 | 现货 | ||
500 mg | ¥ 12,300 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 867 | 现货 |
产品描述 | TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC). |
靶点活性 | APC:50 μM(HCT116 cells), APC:70 nM(DLD1 cells) |
体外活性 | In two authentic human CRC cell lines HCT116 (WT APC) and DLD1 (truncated APC1417), TASIN-1 exhibited potent and selective toxicity toward DLD1 cells (IC50: 70 nM but not toward HCT116 cells (IC50 >50 μM)). TASIN-1 also reduced the endogenous cholesterol biosynthesis rate. TASIN-1 exerted its killing effects primarily by depleting cholesterol through inhibition of emopamil-binding protein (EBP) activity. However, knockdown of truncated APC (>90%) expression desensitized DLD1 cells to TASIN-1, suggesting that APC is required for TASIN-1’s cytotoxicity [1]. |
体内活性 | In nude mice with established DLD1 and HT29 tumors, intraperitoneal injection of TASIN-1 twice daily for 18 days reduced the size of tumor xenografts and tumor growth rates. TASIN-1 resulted in the appearance of apoptotic cells with fragmented nuclei and induced an increase in cleaved caspase 3 and cleaved PARP1. However, TASIN-1 did not inhibit tumor growth in HCT116 xenografts. In a genetically engineered CRC mouse model, TASIN-1 significantly reduced tumor formation in the colons of CPC [1]. |
别名 | 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine, 塔辛-1 |
分子量 | 352.49 |
分子式 | C18H28N2O3S |
CAS No. | 792927-06-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.2 mg/mL
EtOH: 12.02 mg/mL (with ultrasonic)
H2O: 2.45 mg/mL (with gentle warming and ultrasonic)
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。
TASIN-1 792927-06-1 Cell Cycle/Checkpoint APC Inhibitor TASIN1 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine TASIN 1 塔辛-1 inhibit inhibitor