VAL-083

SKU: orb1307627

Description

VAL-083 is a small molecule alkylating agent with antitumor properties, known to induce N7-methylguanine DNA adducts. It is utilized in cancer research for studying DNA damage response mechanisms in both in vitro cell culture and in vivo animal models of glioblastoma and other malignancies.

Research Area

Molecular Biology

Key Properties

• CAS Number: 23261-20-3
• MW: 146.14
• Purity: ≥98% (May vary between batches)
• Formula: C₆H₁₀O₄
• SMILES: [H][C@@]1(CO1)[C@H](O)[C@H](O)[C@]1([H])CO1
• Target: DNA Alkylator/Crosslinker|||DNA Alkylation
• Solubility: DMF:90 mg/mL (615.85 mM);H2O:40 mg/mL (273.71 mM)

Bioactivity

• In Vivo:
  VAL-083 significantly decreases the expression of VEGF, VEGFR2, and FGF2 at a concentration of 25 μg/mL, while at 50 μg/mL, it also reduces FGFR2 expression. Its action involves the activation of the CDC25C-CDK1 cascade in xenografted tumor models. Additionally, VAL-083 exhibits a dose-dependent inhibition of angiogenesis in zebrafish models at concentrations of 25, 50, and 100 μg/mL. In a murine study, VAL-083, administered intravenously at 5 mg/kg twice weekly for six weeks, markedly suppresses LN229 cell growth, resulting in a relative tumor growth rate (T/C) of 22.38% and a tumor growth inhibitory rate (TGI) of 83.58%.
  Read more...
• In Vitro:
  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 .
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Crosslinker, Dianhydrodulcitol, Dianhydrogalactitol, DNA Alkylator/Crosslinker, DNA Alkylator, DNA Alkylation, DNAAlkylator, DNAAlkylation, Inhibitor, inhibit, VAL 083, VAL083, VAL-083

Compound Identifiers

PubChem CID

15942827