Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VT103 是一种具有口服活性和选择性的 TEAD1 蛋白棕榈酰化抑制剂,是 VT101 的类似物。 VT103 有潜在的抗肿瘤活性,可抑制 YAP/TAZ-TEAD 促进的基因转录,阻断 TEAD auto-palmitoylation,阻断 YAP/TAZ和TEAD 之间的相互作用。VT103 可用于研究HER2阳性乳腺癌、前列腺癌和三阴性乳腺癌。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,060 | 现货 | ||
2 mg | ¥ 1,560 | 现货 | ||
5 mg | ¥ 2,650 | 现货 | ||
10 mg | ¥ 4,230 | 现货 | ||
25 mg | ¥ 7,880 | 现货 | ||
50 mg | ¥ 10,800 | 现货 | ||
100 mg | ¥ 14,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,920 | 现货 |
产品描述 | VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP/TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP/TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer. |
体外活性 |
VT103 (3 mmol/L; 4 or 24 h; NF2-deficient NCI-H226 cells) selectively disrupts YAP–TEAD1 interaction.[1] VT103 (3 μM; HEK293T cells) appeared to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4.[1] VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1. VT103 shows an IC50 of 1.02 nM in the YAP reporter assay.[1] |
体内活性 | VT103 (0.3~10 mg/kg; p.o.; once per day; NCI-H226-tumor-bearing mice) blocks tumor growth even at 0.3 mg/kg[1]. Pharmacokinetics of VT103 in mice.[1] |
别名 | VT-103, VT 103 |
分子量 | 410.41 |
分子式 | C18H17F3N4O2S |
CAS No. | 2290608-13-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20.52 mg/mL (50 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4366 mL | 12.1829 mL | 24.3659 mL | 60.9147 mL |
5 mM | 0.4873 mL | 2.4366 mL | 4.8732 mL | 12.1829 mL | |
10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL | 6.0915 mL | |
20 mM | 0.1218 mL | 0.6091 mL | 1.2183 mL | 3.0457 mL | |
50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 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。
VT103 2290608-13-6 Stem Cells YAP VT-103 VT 103 Inhibitor inhibitor inhibit