戊柔比星 T7604

Product Introduction
Bioactivity


英文名: Valrubicin

描述: 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。

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].

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (172.74 mM)
H2O : Insoluble


关键字: Inhibitor | inhibit | Valrubicin | AD 32 | PKC | Antibiotic | Protein kinase C | AD32

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