MAZ51

SKU: orb1220141

Description

MAZ51 is a VEGFR-3 (Flt-4) tyrosine kinase inhibitor. MAZ51 is able to block the proliferation of VEGFR-3-expressing human endothelial cells and is less potently able to induce their apoptosis. MAZ51 also inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.In vivo, MAZ51 significantly inhibits the growth of rat mammary carcinomas. These data establish MAZ51 as a compound with antitumor properties that inhibits tumor growth directly and also indirectly by interfering with tumor-host interactions.

Key Properties

• CAS Number: 163655-37-6
• MW: 314.38
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈N₂O
• SMILES: CN(C)c1ccc(C=C2C(=O)Nc3ccccc23)c2ccccc12
• Target: VEGFR
• Solubility: DMSO:3.33 mg/ml(10.59 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  MAZ51 (8 mg/kg; i.p.; daily for 15 day) significantly suppresses the growth of MT450 tumors. Animal model: Wistar Furth rats (bearing MT450 cells). Dosage: 8 mg/kg. Administration: Intraperitoneal injection; daily for 15 day. Result: Significantly suppressed the growth of MT450 tumors.
• In Vitro:
  MAZ51 (2.5-10 μM; 24 hours) blocks proliferation and induces apoptosis in a wide variety of tumor cells. MAZ51 (0.5-50 μM; 25 minutes) has no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ in A431 cells, HEK-293 cells, and PAE cells, respectively. Cell Proliferation Assay Cell line: MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells Concentration: 2.5, 10 μM Incubation time: 24 hours. Result: Induced apoptosis in a wide variety of tumor cells. Apoptosis Analysis Cell line: MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells Concentration: 2.5, 10 μM Incubation time: 24 hours. Result: Blocked proliferation in a wide variety of tumor cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

VEGFR