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Valrubicin

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Chemical Structure| 56124-62-0 同义名 : AD-32;NSC 246131;Valrubicin, Valstar, Valtaxin, AD 32, AD32, AD-32;N-Trifluoroacetyladriamycin-14-valerate
CAS号 : 56124-62-0
货号 : A191480
分子式 : C34H36F3NO13
纯度 : 99%+
分子量 : 723.644
MDL号 : MFCD01939322
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:
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].
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 <<
实验方案
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

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.