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

VAL-083  (Synonyms: Dianhydrodulcitol; Dianhydrogalactitol)

Cat. No.: HY-16513 Purity: ≥98.0%
COA 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

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 266 In-stock
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10 mM * 1 mL in DMSO USD 266 In-stock
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10 mg USD 150 In-stock
50 mg USD 480 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE VAL-083

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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].

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

Clinical Trial
Molecular Weight

146.14

Formula

C6H10O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@H](O)[C@]1(OC1)[H])[C@@]2([H])CO2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (1368.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : ≥ 100 mg/mL (684.28 mM)

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

*"≥" means soluble, but saturation unknown.

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMF / DMSO 1 mM 6.8428 mL 34.2138 mL 68.4275 mL 171.0688 mL
5 mM 1.3686 mL 6.8428 mL 13.6855 mL 34.2138 mL
10 mM 0.6843 mL 3.4214 mL 6.8428 mL 17.1069 mL
15 mM 0.4562 mL 2.2809 mL 4.5618 mL 11.4046 mL
20 mM 0.3421 mL 1.7107 mL 3.4214 mL 8.5534 mL
25 mM 0.2737 mL 1.3686 mL 2.7371 mL 6.8428 mL
30 mM 0.2281 mL 1.1405 mL 2.2809 mL 5.7023 mL
40 mM 0.1711 mL 0.8553 mL 1.7107 mL 4.2767 mL
50 mM 0.1369 mL 0.6843 mL 1.3686 mL 3.4214 mL
60 mM 0.1140 mL 0.5702 mL 1.1405 mL 2.8511 mL
80 mM 0.0855 mL 0.4277 mL 0.8553 mL 2.1384 mL
100 mM 0.0684 mL 0.3421 mL 0.6843 mL 1.7107 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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VAL-083 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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VAL-083
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