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Valrubicin

Valrubicin

产品编号 T7604   CAS 56124-62-0
别名: Valstar, AD-32, 戊柔比星

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。

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Valrubicin Chemical Structure
Valrubicin, CAS 56124-62-0
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Valrubicin (T7604)
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纯度: 97.41%
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存储 & 溶解度
参考文献
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

存储

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

溶液配制表

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

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TargetMol Library Books参考文献

1. Chuang LF, et al. Activation of human leukemia protein kinase C by tumor promoters and its inhibition by N-trifluoroacetyladriamycin-14-valerate (AD 32). Biochem Pharmacol. 1992 Feb 18;43(4):865-72. 2. Wani MK, et al. Rationale for intralesional valrubicin in chemoradiation of squamous cell carcinoma of the head and neck. Laryngoscope. 2000 Dec;110(12):2026-32. 3. Hauge E, et al. Topical valrubicin application reduces skin inflammation in murine models. Br J Dermatol. 2012 Aug;167(2):288-95.
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相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抑制剂库 TGF-β/Smad靶点化合物库 激酶抑制剂库 药物功能重定位化合物库 抗癌临床化合物库 FDA 上市激酶抑制剂库 抗癌活性化合物库 抗癌上市药物库 表观遗传库

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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。

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Keywords

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

 

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