VAL-083 是一种烷化剂，具有抗肿瘤活性，可在 DNA 上产生 N7 甲基化。

VAL-083 is an alkylating compound that creates N7 methylation on DNA. It also has antitumor activity.

VAL-083 inhibits T98G cell growth in a dose-dependent manner (IC50<5 μM). VAL-083 inhibits the proliferation of HUVEC and U251 cells at doses of more than 12.5 μg/mL. 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 (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 μM) dose-dependently induces cell cycle arrest at the G2/M phase in the 3 glioma cell lines. VAL-083 activates two parallel signaling cascades, the p53-p21, and the CDC25C-CDK1 cascade. VAL-083 significantly enhances the radiosensitivity of LN229 cells [1][2][3].

VAL-083 considerably reduces VEGF, VEGFR2, and FGF2 expression at 25 μg/mL, and further causes a reduction in FGFR2 expression at 50 μg/mL. VAL-083 dramatically activates the CDC25C-CDK1 cascade in the xenografted tumor model. VAL-083 (25, 50, 100 μg/mL) dose-dependently inhibits angiogenesis in the zebrafish model. VAL-083 (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% [2][3].

23261-20-3

C6H10O4

146.14

1,2:5,6-二脱水半乳糖醇;去水卫矛醇;Dianhydrogalactitol;Dianhydrodulcitol

H2O:40 mg/mL (273.71 mM),Need ultrasonic
DMF:90 mg/mL (615.85 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years