VAL-083
(Synonyms: 去水卫矛醇; Dianhydrodulcitol; Dianhydrogalactitol) 目录号 : GC10339
VAL-083 是一种烷化剂，可在 DNA 上产生 N7 甲基化，具有抗肿瘤活性。
Cas No.:23261-20-3
Sample solution is provided at 25 µL, 10mM.
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VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
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].
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].
Reference:
[1]. Kaiji Hu, et al. Abstract 811: VAL083, a novel N7 alkylating agent, surpasses temozolomide 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.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
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. | |
| Cas No. | 23261-20-3 | SDF | |
| 别名 | 去水卫矛醇; Dianhydrodulcitol; Dianhydrogalactitol | ||
| 化学名 | (1S,2R)-1-[(2S)-oxiran-2-yl]-2-[(2R)-oxiran-2-yl]ethane-1,2-diol | ||
| Canonical SMILES | C1C(O1)C(C(C2CO2)O)O | ||
| 分子式 | C6H10O4 | 分子量 | 146.14 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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