| CAS |
No.56124-62-0 |
| 中文名称 |
戊柔比星 |
| 英文名称 |
Valrubicin |
| 分子式 |
C34H36F3NO13 |
| 分子量 |
723.64 |
| 溶解性 |
Soluble in DMSO ≥10mg/mL(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
Orange to red Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| EC |
EINECS 680-664-1 |
| MDL |
MFCD01939322 |
| SMILES |
CCCCC(=O)OCC(=O)C1(CC(C2=C(C1)C(=C3C(=C2O)C(=O)C4=C(C3=O)C=CC=C4OC)O)OC5CC(C(C(O5)C)O)NC(=O)C(F)(F)F)O |
| InChIKey |
ZOCKGBMQLCSHFP-KQRAQHLDSA-N |
| InChI |
InChI=1S/C34H36F3NO13/c1-4-5-9-21(40)49-13-20(39)33(47)11-16-24(19(12-33)51-22-10-17(27(41)14(2)50-22)38-32(46)34(35，36)37)31(45)26-25(29(16)43)28(42)15-7-6-8-18(48-3)23(15)30(26)44/h6-8，14，17，19，22，27，41，43，45，47H，4-5，9-13H2，1-3H3，(H，38，46)/t14-，17-，19-，22-，27+，33-/m0/s1 |
| PubChem CID |
454216 |
| 靶点 |
Others |
| 通路 |
Others |
| 背景说明 |
Valrubicin是一种具有化疗活性的化合物，能够抑制 TPA 和 PDBu 诱导的 PKC 活化，具有抗肿瘤和抗炎活性。 |
| 生物活性 |
Valrubicin is a chemotherapy agent， inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM， respectively， and has antitumor and antiinflammatory activity.[1-3] |
| In Vitro |
Valrubicin (AD 32) 是一种化疗剂，可抑制 TPA 和 PDBu 诱导的 PKC 激活，IC50 分别为 0.85 和 1.25 μM。Valrubicin 抑制[3H]PDBu 与 PKC 的结合。因此，Valrubicin 与肿瘤启动子竞争 PKC 结合位点，并阻止后者与磷脂相互作用和与 PKC 结合[1]。Valrubicin 对鳞状细胞癌 (SCC) 细胞系集落形成具有细胞毒性活性，对于 UMSCC5 的 IC50 和 IC90 分别为 8.24 ± 1.60 μM 和 14.81 ± 2.82 μM细胞，UMSCC5/CDDP? 细胞分别为 15.90 ± 0.90 μM、29.84 ± 0.84 μM，UMSCC10b 细胞分别为 10.50 ± 2.39 μM、19.00 ± 3.91 μM。此外，Valrubicin 联合放疗可增强细胞毒性[2]。 |
| In Vivo |
Valrubicin (3、6 或 9 mg) 在第 3 周通过瘤内注射在仓鼠体内减少肿瘤生长。Valrubicin (6 mg) 与最低限度的细胞毒性辐射 (150、250 或 350 cGy) 相结合可导致仓鼠的肿瘤显著缩小[2]。Valrubicin (0.1 μg/μL) 显著减少 24 小时 TPA 激发的活组织检查中浸润性中性粒细胞的数量，并减轻小鼠的慢性炎症。Valrubicin 还可以降低急性模型中炎性细胞因子的表达水平[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 phosphate-buffered saline (PBS)， and fixed at 5 × 106 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[2]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; 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[2]. |
| 数据来源文献 |
[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. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
中文
英语
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