1. Cell Cycle/DNA Damage
  2. DNA Alkylator/Crosslinker
  3. VAL-083

VAL-083 (Synonyms: Dianhydrodulcitol; Dianhydrogalactitol)

Cat. No.: HY-16513 Purity: >98.0%
Handling Instructions

VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.

For research use only. We do not sell to patients.

VAL-083 Chemical Structure

VAL-083 Chemical Structure

CAS No. : 23261-20-3

Size Price Stock Quantity
10 mM * 1 mL in Water USD 370 In-stock
Estimated Time of Arrival: December 31
5 mg USD 336 In-stock
Estimated Time of Arrival: December 31
10 mg USD 432 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1164 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.

IC50 & Target

DNA Alkylator[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (342.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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 0.6843 mL 3.4214 mL 6.8428 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

146.14

Formula

C₆H₁₀O₄

CAS No.

23261-20-3

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
VAL-083
Cat. No.:
HY-16513
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VAL-083

Cat. No.: HY-16513