中文名称: 戊柔比星
英文名称: Valrubicin
CAS No: 56124-62-0
分子式: C34H36F3NO13
分子量: 723.64
V10124 戊柔比星 ≥98% (psaitong)
包装规格:
50mg 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℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):