[CAS NO. 23261-20-3] VAL-083
PRODUCTS SPECIFICATIONS [23261-20-3]
DESCRIPTION [23261-20-3]
Overview
| MDL | MFCD01725532 |
|---|---|
| Molecular Weight | 146.14 |
| Molecular Formula | C6H10O4 |
| SMILES | O[C@H]([C@H](O)[C@]1(OC1)[H])[C@@]2([H])CO2 |
1 Publications Citing Use of MCE
Summary
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 (IC 50 <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] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03970447 | Global Coalition for Adaptive Research|Bayer|Kazia Therapeutics Limited|Kintara Therapeutics, Inc.|Biohaven Pharmaceuticals, Inc.|Vigeo Therapeutics, Inc. |
Glioblastoma
|
July 30, 2019 | Phase 2|Phase 3 |
| NCT03149575 | DelMar Pharmaceuticals, Inc.|Kintara Therapeutics, Inc. |
Glioblastoma Multiforme|Glioblastoma|Glioma|GBM|Brain Cancer
|
October 27, 2017 | Phase 3 |
| NCT02717962 | Kintara Therapeutics, Inc. |
Glioma|Glioblastoma|Glioblastoma Multiforme|GBM|Brain Cancer
|
January 20, 2017 | Phase 2 |
| NCT03281681 | DelMar Pharmaceuticals, Inc.|Kintara Therapeutics, Inc. |
Ovarian Cancer
|
March 2021 | Phase 1|Phase 2 |
| NCT01478178 | DelMar Pharmaceuticals, Inc.|Kintara Therapeutics, Inc. |
Glioma|Glioblastoma|Glioblastoma Multiforme|GBM|Brain Cancer
|
October 2011 | Phase 1|Phase 2 |
| NCT03050736 | Kintara Therapeutics, Inc.|Sun Yat-sen University |
Glioma|Glioblastoma|Glioblastoma Multiforme|GBM|Brain Cancer
|
December 17, 2017 | Phase 2 |
| NCT03138629 | Kintara Therapeutics, Inc. |
Cancer
|
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 200 mg/mL ( 1368.55 mM ; ultrasonic and warming and heat to 60°C)
DMF : ≥ 100 mg/mL ( 684.28 mM )
H 2 O : 50 mg/mL ( 342.14 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 |
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.
- [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.
Synonyms