戊柔比星
中文名称:
戊柔比星
中文同义词:
戊柔比星;戊柔吡星;戊柔比星(比星类);戊柔比星 USP标准品;戊柔比星(RD)
英文名称:
Valrubicin
英文同义词:
ad32;antibioticad32;nsc-246131;n-trifluoroacetyladriamycin-14-valerate;n-trifluoroacetyladriamycin14-valerate;n-trifluoroacetyldoxorubicin14-valerate;trifluoroacetyl-adriamyci14-valerate;trifluoroacetyladriamycin-14-valerate
CAS号:
56124-62-0
分子式:
C34H36F3NO13
分子量:
723.64
EINECS号:
680-664-1
相关类别:
BICINS比星类产品(Anti-cancer);医药原料药;医药中间体;科研原药系列;原料药【仅供科研】;医药原料;抗肿瘤;Antineoplastic;Intermediates Fine Chemicals;Pharmaceuticals;API;原料;抗癌药
Mol文件:
56124-62-0.mol
熔点
116-117 °C
沸点
135-136 C
密度
1.3473 (estimate)
储存条件
Sealed in dry,2-8°C
酸度系数(pKa)
7.34±0.60(Predicted)
水溶解性
insoluble
生物活性
Valrubicin 是一种化疗药物，用于治疗膀胱癌。Valrubicin 可抑制 TPA- 和 PDBu- 诱导的 PKC 活化，对应的IC50值分别为0.85 μM 和 1.25 μM。
靶点
Target Value
TPA-activated PKC
(Cell-free assay) 0.85 μM
PDBu-activated PKC
(Cell-free assay) 1.25 μM
Target
Value
TPA-activated PKC
(Cell-free assay)
0.85 μM
PDBu-activated PKC
(Cell-free assay)
1.25 μM
体外研究
Valrubicin (AD 32) is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC 50 s of 0.85 and 1.25 μM, respectively. Valrubicin inhibits the binding of [ 3 H]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 IC 50 s and IC 90 s of 8.24 ± 1.60 μM and 14.81 ± 2.82 μM for UMSCC5 cells, 15.90 ± 0.90 μM, 29.84 ± 0.84 μM for UMSCC5/CDDP‡ cells, and 10.50 ± 2.39 μM, 19.00 ± 3.91 μM for UMSCC10b cells, respectively. Moreover, Valrubicin in combination with radiation enhances the cytotoxicity.
体内研究
Valrubicin (3, 6, or 9 mg) reduces tumor growth at week 3 by intratumoral jection in hamster. Valrubicin (6 mg) combined with minimally cytotoxic irradiation (150, 250, or 350 cGy) causes significant tumor shrinkage in hamster. 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.
危险品标志
Xi
危险类别码
36/37/38
安全说明
26-37/39
海关编码
2941906000
毒害物质数据
56124-62-0(Hazardous Substances Data)
毒性
dnd-hmn:lym 3 mg/L CJBIAE 58,720,80
