产品描述: | VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity. |
靶点: |
DNA Alkylator;DNAAlkylator/Crosslinker; DNAAlkylation |
体内研究: |
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. 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 |
参考文献: |
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. |
溶解性: |
DMSO : 200 mg/mL (1368.55 mM; ultrasonic and warming and heat to 60°C) DMF : ≥ 100 mg/mL (684.28 mM) H2O : 50 mg/mL (342.14 mM; Need ultrasonic) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
6.843 ml |
34.214 ml |
68.428 ml |
5 mM |
1.369 ml |
6.843 ml |
13.686 ml |
10 mM |
0.684 ml |
3.421 ml |
6.843 ml |
50 mM |
0.137 ml |
0.684 ml |
1.369 ml |
|
注意: |
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