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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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ellagic acid | ✔ | 99%+ | |||||||||||||||||
β-Lapachone | ✔ | 99%+ | |||||||||||||||||
(s)-10-hydroxycamptothecin | ✔ | 99%+ | |||||||||||||||||
Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
99%+ | |||||||||||||||||
Topotecan |
++++
Topo I (DU-145 Luc cells), IC50: 2 nM Topo I (MCF-7 Luc cells), IC50: 13 nM |
99%+ | |||||||||||||||||
Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
SN-38 | ✔ | 98% | |||||||||||||||||
Levofloxacin hydrate | ✔ | 99%+ | |||||||||||||||||
Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
Ofloxacin | ✔ | 98+% | |||||||||||||||||
Enoxacin | ✔ | 99%+ | |||||||||||||||||
Flumequine |
+
Topo II, IC50: 15 μM |
99%+ | |||||||||||||||||
Levofloxacin | ✔ | 99%+ | |||||||||||||||||
Etoposide | ✔ | 98% | |||||||||||||||||
Pefloxacin mesylate dihydrate | ✔ | 99+% | |||||||||||||||||
Marbofloxacin | ✔ | 99%+ | |||||||||||||||||
Voreloxin HCl | ✔ | 98% | |||||||||||||||||
Mitoxantrone dihydrochloride | ✔ | PKC | 99%+ | ||||||||||||||||
Nalidixic acid | ✔ | 99%+ | |||||||||||||||||
Doxorubicin | ✔ | 98% | |||||||||||||||||
Novobiocin sodium | ✔ | 98%+ | |||||||||||||||||
Amonafide | ✔ | 99%+ | |||||||||||||||||
Pirarubicin | ✔ | 98%+ | |||||||||||||||||
Idarubicin HCl |
+++
Topo II (MCF-7 cells), IC50: 3.3 ng/mL |
99%+ | |||||||||||||||||
Genistein | ✔ | EGFR | 98% | ||||||||||||||||
Teniposide | ✔ | 98% | |||||||||||||||||
Moxifloxacin | ✔ | 98% | |||||||||||||||||
Ciprofloxacin | ✔ | 99%+ | |||||||||||||||||
Clinafloxacin | ✔ | 97% | |||||||||||||||||
Gatifloxacin | ✔ | 99%+ | |||||||||||||||||
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。 |
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]. |
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 << |
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 |
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 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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 |
动物实验配方 |