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VAL-083

Catalog No. T17212   CAS 23261-20-3
Synonyms: Dianhydrogalactitol, Dianhydrodulcitol

VAL-083 (Dianhydrogalactitol) is an alkylating compound that creates N7 methylation on DNA. It also has antitumor activity.

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VAL-083 Chemical Structure
VAL-083, CAS 23261-20-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 80.00
2 mg In stock $ 119.00
5 mg In stock $ 182.00
10 mg In stock $ 247.00
25 mg In stock $ 415.00
50 mg In stock $ 617.00
100 mg In stock $ 878.00
1 mL * 10 mM (in DMSO) In stock $ 156.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description VAL-083 (Dianhydrogalactitol) is an alkylating compound that creates N7 methylation on DNA. It also has antitumor activity.
In vitro VAL-083 inhibits T98G cell growth in a dose-dependent manner (IC50 <5 μM). VAL-083 inhibits the proliferation of HUVEC and U251 cells at doses of more than 12.5 μg/mL. 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 (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. VAL-083 (1, 2, 5 μM) dose-dependently induces cell cycle arrest at the G2/M phase in the 3 glioma cell lines. VAL-083 activates two parallel signaling cascades, the p53-p21, and the CDC25C-CDK1 cascade. VAL-083 significantly enhances the radiosensitivity of LN229 cells [1][2][3].
In vivo VAL-083 significantly decreases the expression of VEGF, VEGFR2, and FGF2 at a concentration of 25 μg/mL, while at 50 μg/mL, it also reduces FGFR2 expression. Its action involves the activation of the CDC25C-CDK1 cascade in xenografted tumor models. Additionally, VAL-083 exhibits a dose-dependent inhibition of angiogenesis in zebrafish models at concentrations of 25, 50, and 100 μg/mL. In a murine study, VAL-083, administered intravenously at 5 mg/kg twice weekly for six weeks, markedly suppresses LN229 cell growth, resulting in a relative tumor growth rate (T/C) of 22.38% and a tumor growth inhibitory rate (TGI) of 83.58%.
Synonyms Dianhydrogalactitol, Dianhydrodulcitol
Molecular Weight 146.14
Formula C6H10O4
CAS No. 23261-20-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 40 mg/mL (273.71 mM), sonification is recommended.

DMF: 90 mg/mL (615.85 mM)

TargetMolReferences and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Preclinical Compound Library Covalent Inhibitor Library Human Metabolite Library ReFRAME Related Library Approved Drug Library

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Keywords

VAL-083 23261-20-3 DNA Damage/DNA Repair DNA Alkylator/Crosslinker DNA Alkylation VAL083 VAL 083 Inhibitor inhibit Dianhydrogalactitol Dianhydrodulcitol inhibitor

 

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