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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥130mg/mL）
产品描述：基本信息 产品编号：V10124 产品名称：Valrubicin CAS: 56124-62-0   储存条件 粉末 -20℃ 四年     分子式： C34H36F3NO13 溶于液体 -80℃ 六个月 分子量： 723.64 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (138.19mM) Ethanol 100mg/mL (138.19mM) Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.3819mL 6.9095mL 13.8190mL 5mM 0.2764mL 1.3819mL 2.7638mL 10mM 0.1382mL 0.6910mL 1.3819mL 50mM 0.0276mL 0.1382mL 0.2764mL   生物活性 产品描述 一种化疗剂，能够抑制 TPA 和 PDBu 诱导的 PKC 活化，IC50 值分别为 0.85 和 1.25μM，具有抗肿瘤和抗炎作用。 靶点/IC50 TPA-activated PKC (Cell-free assay) PDBu-activated PKC (Cell-free assay) 0.85μM 1.25μM   体外研究 Valrubicin (AD 32) is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25μM,respectively. 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. Valrubicin shows cytotoxic activity against squamous cell carcinoma (SCC) cell line colony formation, with IC50s and IC90s of 8.24±1.60μM and 14.81±2.82μM for UMSCC5 cells, 15.90 ± 0.90μM, 29.84±0.84μM for UMSCC5/CDDP‡ cells, and 10.50±2.39μM,19.00±3.91μM for UMSCC10b cells,respectively. Moreover, Valrubicin in combination with radiation enhances the cytotoxicity. 体内研究 Valrubicin (3, 6, or 9mg) reduces tumor growth at week 3 by intratumoral jection in hamster.Valrubicin (6mg) combined with minimally cytotoxic irradiation (150, 250,or 350 cGy) causes significant tumor shrinkage in hamster. Valrubicin (0.1μg/μL) significantly reduces the number of infiltrating neutrophils in biopsies challenged with TPA at 24h and attenuates chronic inflammation in mice. Valrubicin also decreases the expression levels of inflammatory cytokines in the acute model.   推荐实验方法(仅供参考) 细胞实验:   UMSCC5 cells exposed to Valrubicin (2μM for 3h), a single dose of radiation (400 cGy), or the combined treatment are cultured for a further 12, 24, or 48hours. At these times, the cells are collected by trypsinization (0.25%), washed in phosphate-buffered saline (PBS), and fixed at 5 × 106 cells/mL with 95% ethanol. Cells are incubated with ribonuclease (50μg; 70-90 Kunitz units/mg for 30 min), and the resulting pellet resuspended in and incubated with propidium iodide (0.05mg/mL for 10 min). The DNA content of the samples is determined by flow cytometry according to standard technique.   动物实验:   Hamsters Hamsters with cheek pouch tumors of 100mm2 are randomly assigned to one of five treatment groups. Momentarily anesthetized animals each receives once a week× 3 injections (27g×0.5-inch needle: 0.1mL administered slowly to the base of the lesion) of Valrubicin (3, 6, or 9mg) or drug vehicle (Cremophor: alcohol;1:1 by volume; NCl 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.
保存条件：-20℃

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