Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Valrubicin (AD-32) 是一种具有抗炎和抗肿瘤作用的化疗剂,能够抑制 TPA 和 PDBu 诱导的 PKC 活化,IC50值分别为 0.85 和 1.25 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 445 | 现货 | ||
5 mg | ¥ 1,080 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 2,690 | 现货 | ||
50 mg | ¥ 3,960 | 现货 | ||
100 mg | ¥ 5,650 | 现货 |
产品描述 | Valrubicin (AD-32) (AD 32) inhibits TPA- and PDBu-induced PKC activation (IC50s: 0.85 and 1.25 μM) and has antitumor and anti-inflammatory activity. |
靶点活性 | PKC (TPA-activated):0.85 μM, PKC (PDBu-induced):1.25 μM |
体外活性 | Valrubicin inhibits the binding of [3H]PDBu to PKC. Therefore, Valrubicin competes with the tumor promoter for the PKC binding site and prevents the latter from both interacting with the phospholipid and binding to PKC [1]. Valrubicin shows cytotoxic activity against squamous cell carcinoma (SCC) cell line colony formation, with IC50s and IC90s of 8.24 μM and 14.81 μM for UMSCC5 cells, 15.90 μM, 29.84 μM for UMSCC5/CDDP? cells, and 10.50 μM, 19.00 μM for UMSCC10b cells, respectively [2]. |
体内活性 | Valrubicin (3, 6, or 9 mg) reduces tumor growth at week 3 by intratumoral injection in the hamster. Valrubicin (6 mg) combined with minimally cytotoxic irradiation (150, 250, or 350 cGy) causes significant tumor shrinkage in the hamster [2]. Valrubicin (0.1 μg/μL) significantly reduces the number of infiltrating neutrophils in biopsies challenged with TPA at 24 h and attenuates chronic inflammation in mice. Valrubicin also decreases the expression levels of inflammatory cytokines in the acute model [3]. |
细胞实验 | UMSCC5 cells exposed to Valrubicin (2 μM for 3 h), a single dose of radiation (400 cGy), or the combined treatment are cultured for a further 12, 24, or 48 hours. At these times, the cells are collected by trypsinization (0.25%), washed in PBS, and fixed at 5 × 10^6 cells/mL with 95% ethanol. Cells are incubated with ribonuclease (50 μg; 70-90 Kunitz units/mg for 30 min), and the resulting pellet resuspended in and incubated with propidium iodide (0.05 mg/mL for 10 min). The DNA content of the samples is determined by flow cytometry according to standard technique [2]. |
动物实验 | Hamsters with cheek pouch tumors of 100 mm2 are randomly assigned to one of five treatment groups. Momentarily anesthetized animals each receives once a week × 3 injections (27 g × 0.5-inch needle: 0.1 mL administered slowly to the base of the lesion) of Valrubicin (3, 6, or 9 mg) or drug vehicle (Cremophor: alcohol;1:1 by volume; NaCl diluent 12). A further group of animals receives anesthesia but no direct tumor treatment (control). Individual tumor sizes are measured with calipers at weekly intervals for 4 weeks, at which time the animals are sacrificed [2]. |
别名 | Valstar, AD-32, 戊柔比星 |
分子量 | 723.64 |
分子式 | C34H36F3NO13 |
CAS No. | 56124-62-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (172.74 mM)
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3819 mL | 6.9095 mL | 13.819 mL | 34.5476 mL |
5 mM | 0.2764 mL | 1.3819 mL | 2.7638 mL | 6.9095 mL | |
10 mM | 0.1382 mL | 0.691 mL | 1.3819 mL | 3.4548 mL | |
20 mM | 0.0691 mL | 0.3455 mL | 0.691 mL | 1.7274 mL | |
50 mM | 0.0276 mL | 0.1382 mL | 0.2764 mL | 0.691 mL | |
100 mM | 0.0138 mL | 0.0691 mL | 0.1382 mL | 0.3455 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。
Valrubicin 56124-62-0 Chromatin/Epigenetic Cytoskeletal Signaling Microbiology/Virology Antibiotic PKC Inhibitor Valstar inhibit AD-32 AD 32 戊柔比星 Protein kinase C AD32 inhibitor