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| ln Vitro |
N7 methylation of DNA is produced by the alkylating chemical VAL-083. After 72 hours, VAL-083 stimulates cell proliferation while inhibiting that of U251 and SF188. SF188 growth is inhibited by VAL-083 (5 μM) by almost 95%. T98G cell proliferation is dose-dependently inhibited by VAL-083 (IC50 <5 μM)[1]. At concentrations more than 12.5 μg/mL, VAL-083 (dihydrogalactitol) inhibits the growth of HUVEC and U251 cells. In HUVEC and U251 cells, VAL -083 (3.125, 6.25, 12.5 μg/mL) also decreases MMP2, VEGF, VEGFR2, and FGF2 production in addition to inhibiting migration and threshold [2]. In three neuroastrocytoma cells, VAL-083 (1,2:5,6-dianhydrogalactitol, 1,2,5 μM) dose-dependently initiates the cell cycle in the G2/M phase. The two parallel signaling cascades that VAL-083 activates are the CDC25C-CDK1 and p53-p21 cascades. Furthermore, VAL-083 markedly improved LN229's ability to target cellular radiation [3].
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| ln Vivo |
In zebrafish models, VAL-083 (DianHydrgalactitol; 25, 50, and 100 μg/mL) quantitatively suppresses angiogenesis. At 25 μg/mL, VAL-083 dramatically lowers the expression of VEGF, VEGFR2, and FGF2, and at 50 μg/mL, it further reduces the expression of FGFR2 [2]. The growth of mice LN229 cells is markedly inhibited by VAL-083 (1,2:5,6-divided galactitol; 5 mg/kg, intravenously, twice a week for 6 weeks), as compared to tumor growth rate (T/C) of 22.38% and tumor growth inhibition rate (TGI) of 83.58%. Furthermore, in xenograft tumor models, VAL-083 markedly activates the CDC25C-CDK1 cascade [3].
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| References |
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| Additional Infomation |
Dianhydrogalactitol has been used in trials studying the treatment of GBM, Glioma, Glioblastoma, Brain Cancer, and Glioblastoma Multiforme.
Dianhydrogalactitol is a bifunctional hexitol derivative with potential antineoplastic activity. Dianhydrogalactitol alkylates and cross-links DNA via an epoxide group during all phases of the cell cycle, resulting in disruption of DNA function and cell cycle arrest. (NCI04) One of the cytotoxic dihalohexitols that alkylates and cross-links DNA via an epoxide group during all phases of the cell cycle, resulting in a disruption of DNA function and cell cycle arrest. It has antineoplastic activity and also causes bone marrow toxicity. |
| Molecular Formula |
C6H10O4
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|---|---|
| Molecular Weight |
146.14
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| Exact Mass |
146.058
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| CAS # |
23261-20-3
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| PubChem CID |
15942827
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| Appearance |
White to off-white solid powder
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| Density |
1.567
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| Boiling Point |
348ºC at 760mmHg
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| Flash Point |
164.3ºC
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| LogP |
-1.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
10
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| Complexity |
122
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1[C@@H](O1)[C@@H]([C@@H]([C@@H]2CO2)O)O
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| InChi Key |
AAFJXZWCNVJTMK-GUCUJZIJSA-N
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| InChi Code |
InChI=1S/C6H10O4/c7-5(3-1-9-3)6(8)4-2-10-4/h3-8H,1-2H2/t3-,4+,5+,6-
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| Chemical Name |
(1S,2R)-1-[(2S)-oxiran-2-yl]-2-[(2R)-oxiran-2-yl]ethane-1,2-diol
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| Synonyms |
VAL083; VAL083; VAL083
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| HS Tariff Code |
2934.99.9001
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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 : ~200 mg/mL (~1368.55 mM)
DMF :≥ 100 mg/mL (~684.28 mM) H2O : ~50 mg/mL (~342.14 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
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