Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Valrubicin is a semisynthetic analogue of the antineoplastic anthracycline antibiotic doxorubicin. With a mechanism of action that appears to differ from doxorubicin, valrubicin is converted intracytoplasmically into N-trifluoroacetyladriamycin, which interacts with topoisomerase II, stabilizing the complex between the enzyme and DNA; consequently, DNA replication and repair and RNA and protein synthesis are inhibited and the cell cycle is arrested in the G2 phase. In addition, this agent accumulates in the cell cytoplasm where it inhibits protein kinase C (PKC). Valrubicin is less cardiotoxic than doxorubicin when administered systemically; applied topically, this agent shows excellent tissue penetration.
ln Vitro |
The modulator valrubicin (AD 32) has an IC50 of 0.85 μM and 1.25 μM, respectively, and inhibits PKC activation produced by TPA and PDBu. Valrubicin prevents [3H]PDBu from attaching itself to PKC. As a result, tumor promoters and valrubicin compete for PKC binding. Valrubicin exhibits cytotoxic effect against colonies of squamous cell carcinoma (SCC) cell line, as seen by its IC50 and IC90 values for UMSCC5 cells, which are 8.24 ± 1.60 μM and 14.81 ± 2.82 μM, respectively. /CDDP The cells had respective concentrations of 15.90 ± 0.90 μM and 29.84 ± 0.84 μM, while the UMSCC10b cells had concentrations of 10.50 ± 2.39 μM and 19.00 ± 3.91 μM. Furthermore, valrubicin plus radiation therapy can increase cytotoxicity [2].
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ln Vivo |
By intraperitoneal administration, valrubicin (3, 6, or 9 mg) inhibited tumor growth in hamsters at week three. In hamsters, valrubicin (6 mg) in combination with low doses of cytotoxic radiation (150, 250, or 350 cGy) caused developing tumors to significantly decrease [2]. In mice with 24-hour TPA-challenged biopsies, valrubicin (0.1 μg/μL) dramatically lowers the amount of active neutrophils and decreases chronic inflammation. In acute settings, valrubicin can also lower the amounts of inflammatory cytokine expression [3].
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References |
[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 |
Molecular Formula |
C34H36F3NO13
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Molecular Weight |
723.64
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CAS # |
56124-62-0
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Related CAS # |
56124-62-0;
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SMILES |
CCCCC(OCC([C@]1(O)CC2=C(C(O)=C3C(C4=C(C(C3=C2O)=O)C=CC=C4OC)=O)[C@@H](O[C@H]5C[C@H](NC(C(F)(F)F)=O)[C@H](O)[C@H](C)O5)C1)=O)=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~125 mg/mL (~172.74 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (3.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3819 mL | 6.9095 mL | 13.8190 mL | |
5 mM | 0.2764 mL | 1.3819 mL | 2.7638 mL | |
10 mM | 0.1382 mL | 0.6910 mL | 1.3819 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.