VAL-083 |
Catalog No.GC10339
One-Click Copy Product Info
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 23261-20-3
Sample solution is provided at 25 µL, 10mM.
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VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
VAL-083 is an alkylating agent that creates N7 methylation on DNA. VAL-083 suppresses U251 and SF188 cell growth and induces apoptosis after 72 h. VAL-083 (5 μM) inhibits the growth of SF188 by ∼95%. VAL-083 inhibits T98G cells growth in a dose-dependent manner (IC50 <5 μM)[1]. VAL-083 (Dianhydrogalactitol) inhibits the proliferation of HUVEC and U251 cells at doses of more than 12.5 μg/mL. VAL-083 (3.125, 6.25, 12.5 μg/mL) also suppresses the migration and invasion, and reduces MMP2, VEGF, VEGFR2, and FGF2 expression in HUVEC and U251 cells[2]. VAL-083 (1,2:5,6-dianhydrogalactitol, 1, 2, 5 μM) dose-dependently induces cell cycle arrest at G2/M phase in the 3 glioma cell lines. VAL-083 activates two parallel signaling cascades, the p53-p21 and the CDC25C-CDK1 cascade. In addition, VAL-083 significantly enhances the radiosensitivity of LN229 cells[3].
VAL-083 (Dianhydrogalactitol; 25, 50, 100 μg/mL) dose-dependently inhibits angiogenesis in zebrafish model. VAL-083 considerably reduces VEGF, VEGFR2, and FGF2 expression at 25 μg/mL, and further causes reduction in FGFR2 expression at 50 μg/mL[2]. VAL-083 (1,2:5,6-dianhydrogalactitol; 5 mg/kg, iv, twice per week for 6 weeks) significantly blocks the growth of LN229 cells in mice with the relative tumor growth rate (T/C) of 22.38%, and the tumor growth inhibitory rate (TGI) of 83.58%. Moreover, VAL-083 dramatically activates the CDC25C-CDK1 cascade in the xenografted tumor moedl[3].
Reference:
[1]. Kaiji Hu, et al. Abstract 811: VAL083, a novel N7 alkylating agent, surpasses temozolomide activity and inhibits cancer stem cells providing a new potential treatment option for glioblastoma multiforme. Cancer Research. 2012 Mar 31-Apr 4.
[2]. Jiang X, et al. Dianhydrogalactitol, a potential multitarget agent, inhibits glioblastoma migration, invasion, and angiogenesis. Biomed Pharmacother. 2017 Jul;91:1065-1074.
[3]. Peng C, et al. 1,2:5,6-dianhydrogalactitol inhibits human glioma cell growth in vivo and in vitro by arresting the cell cycle at G2/M phase. Acta Pharmacol Sin. 2017 Apr;38(4):561-570.
Cell experiment: | The effects of VAL-083 in HUVEC and U251 cellHUVEC and U251 cell proliferation are measured by the CCK8 assay. Cells are seeded into 96-well plates at a destiny of 1 × 104 cells per well. After overnight incubation, cell attachment is followed by the addition of VAL-083 in various concentrations for 24 h; then 10 μL CCK8 is added to each well and incubated at 37°C for 2 h. Optical density is measured at 450 nm[2]. |
Animal experiment: | Mice[3]LN229 cells are suspended in MEM, and 2 × 106 cells per mouse are subcutaneously injected into the flank of BALB/c nude mice at 6-8 weeks old. The tumor volume is calculated as follows: 0.5×L×W2. Tumor-bearing mice are divided into two groups (n = 8) with similar average volumes (vehicle: 108 ± 4 mm3 vs VAL-083: 107 ± 4 mm3). Then, both groups undergo the following treatment: The VAL-083 treatment group receives VAL-083 at 5 mg/kg or 10 μL/g, iv, twice per week for 6 weeks. The vehicle group receives saline at 10 μL/g, iv, three times per week for 6 weeks. Tumor volumes are measured twice per week[3]. |
References: [1]. Kaiji Hu, et al. Abstract 811: VAL083, a novel N7 alkylating agent, surpasses NSC 362856 activity and inhibits cancer stem cells providing a new potential treatment option for glioblastoma multiforme. Cancer Research. 2012 Mar 31-Apr 4. | |
| Cas No. | 23261-20-3 | SDF | |
| Chemical Name | (1S,2R)-1-[(2S)-oxiran-2-yl]-2-[(2R)-oxiran-2-yl]ethane-1,2-diol | ||
| Canonical SMILES | C1C(O1)C(C(C2CO2)O)O | ||
| Formula | C6H10O4 | M.Wt | 146.14 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.8428 mL | 34.2138 mL | 68.4275 mL |
| 5 mM | 1.3686 mL | 6.8428 mL | 13.6855 mL |
| 10 mM | 684.3 μL | 3.4214 mL | 6.8428 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)