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戊柔比星 /Valrubicin {[allProObj[0].p_purity_real_show]}

货号:A191480 同义名: AD-32;NSC 246131

Valrubicin是一种化疗药物,其对TPA-和PDBu诱导的PKC激活具有0.85和1.25 μM的IC50值,具有抗癌和抗炎性能。

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Valrubicin 化学结构 CAS号:56124-62-0
Valrubicin 化学结构
CAS号:56124-62-0
Valrubicin 3D分子结构
CAS号:56124-62-0
Valrubicin 化学结构 CAS号:56124-62-0
Valrubicin 3D分子结构 CAS号:56124-62-0
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Valrubicin 纯度/质量文件 产品仅供科研

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Topo I, IC50: 0.68 μM

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Topo I (MCF-7 Luc cells), IC50: 13 nM

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98%
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Dexrazoxane 99%+
Ofloxacin 98+%
Enoxacin 99%+
Flumequine +

Topo II, IC50: 15 μM

98%
Levofloxacin 97%
Etoposide 98%
Pefloxacin mesylate dihydrate 99+%
Marbofloxacin 98+%
Voreloxin HCl 98%
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Nalidixic acid 98%
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Amonafide 99%+
Pirarubicin 98%+
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Topo II (MCF-7 cells), IC50: 3.3 ng/mL

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Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Epirubicin HCl 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Valrubicin 生物活性

描述 Valrubicin (AD 32) is a chemotherapy agent that inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. Valrubicin competes with the tumor promoter for the PKC binding site, preventing its interaction with phospholipids and binding to PKC [1]. Valrubicin exhibits cytotoxicity against squamous cell carcinoma (SCC) cell line colony formation, with IC50s and IC90s of 8.24 ± 1.60 μM and 14.81 ± 2.82 μM for UMSCC5 cells, 15.90 ± 0.90 μM and 29.84 ± 0.84 μM for UMSCC5/CDDP‡ cells, and 10.50 ± 2.39 μM and 19.00 ± 3.91 μM for UMSCC10b cells, respectively. Additionally, the combination of Valrubicin with radiation enhances cytotoxicity [2].
体内研究

Valrubicin, administered via intratumoral injection at doses of 3, 6, or 9 mg, decreases tumor growth by week 3 in hamsters. Combining Valrubicin at a dose of 6 mg with minimally cytotoxic irradiation (150, 250, or 350 cGy) induces substantial tumor shrinkage in hamsters [2].

Valrubicin (0.1 μg/μL) markedly reduces the infiltration of neutrophils in TPA-challenged biopsies after 24 hours and mitigates chronic inflammation in mice. Additionally, Valrubicin lowers the expression levels of inflammatory cytokines in the acute model [3].

体外研究

Valrubicin (AD 32) is a chemotherapy agent that inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. Valrubicin competes with the tumor promoter for the PKC binding site, preventing its interaction with phospholipids and binding to PKC [1].

Valrubicin exhibits cytotoxicity against squamous cell carcinoma (SCC) cell line colony formation, with IC50s and IC90s of 8.24 ± 1.60 μM and 14.81 ± 2.82 μM for UMSCC5 cells, 15.90 ± 0.90 μM and 29.84 ± 0.84 μM for UMSCC5/CDDP‡ cells, and 10.50 ± 2.39 μM and 19.00 ± 3.91 μM for UMSCC10b cells, respectively. Additionally, the combination of Valrubicin with radiation enhances cytotoxicity [2].

Valrubicin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02256098 Osteoarthritis Arthritis ... 展开 >> Joint Diseases Musculoskeletal Diseases Rheumatic Diseases 收起 << Not Applicable Completed - Netherlands ... 展开 >> Medisch Centrum Haaglanden Den Haag, Netherlands, 2501CK Leiden University Medical Center Leiden, Netherlands, 2300RC 收起 <<
NCT02269254 Osteoarthritis Arthritis ... 展开 >> Joint Diseases Musculoskeletal Diseases Rheumatic Diseases 收起 << Not Applicable Enrolling by invitation February 2019 Netherlands ... 展开 >> Leiden University Medical Center Leiden, Netherlands, 2300RC 收起 <<
NCT00003759 Bladder Cancer Phase 2 Completed - United States, Texas ... 展开 >> University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030-4009 收起 <<

Valrubicin 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.

Valrubicin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.38mL

0.28mL

0.14mL

6.91mL

1.38mL

0.69mL

13.82mL

2.76mL

1.38mL

Valrubicin 技术信息

CAS号56124-62-0
分子式C34H36F3NO13
分子量 723.644
别名 AD-32;NSC 246131;Valrubicin, Valstar, Valtaxin, AD 32, AD32, AD-32;N-Trifluoroacetyladriamycin-14-valerate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 120 mg/mL(165.83 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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