1,2:5,6-二脱水半乳糖醇

生物活性靶点体外研究体内研究 1,2:5,6-二脱水半乳糖醇试剂级价格

1,2:5,6-二脱水半乳糖醇

CAS号:23261-20-3
英文名:Dianhydrogalactitol
中文名:1,2:5,6-二脱水半乳糖醇
CBNumber:CB41016710
分子式:C6H10O4
分子量:146.14
MOL File:23261-20-3.mol

1,2:5,6-二脱水半乳糖醇化学性质

熔点 :96.5-98.5 °C
沸点 :185.74°C (rough estimate)
密度 :1.567
折射率 :1.4310 (estimate)
储存条件 :Store at -20°C
溶解度 :Soluble in DMSO
形态 :Powder
酸度系数(pKa) :13.53±0.20(Predicted)
颜色 :White to off-white

1,2:5,6-二脱水半乳糖醇性质、用途与生产工艺

生物活性 VAL-083 是一种烷化剂 (alkylator)，能够在 DNA 上产生 N7 甲基化，具有抗肿瘤活性。
靶点

DNA Alkylator
体外研究

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). 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. 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.
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.