Molecular Formula | C21H18N2O |
Molar Mass | 314.38 |
Solubility | DMSO: 11mg/mL |
Appearance | solid |
Color | orange |
Storage Condition | 2-8°C |
In vitro study | 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. |
In vivo study | 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. |
Risk Codes | R22 - Harmful if swallowed R37/38 - Irritating to respiratory system and skin. R41 - Risk of serious damage to eyes R51/53 - Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S39 - Wear eye / face protection. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9/PG 3 |
biological activity | MAZ51 is a selective vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) potent inhibitors of tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest of glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 can inhibit the proliferation and induce apoptosis of a variety of non VEGFR-3 expressing tumor cells. |
Target | TargetValue VEGFR-3 () Akt () GSK3β () RhoA () |
Target | Value |
in vitro study | 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 auto-phosphate of EGFR, IGF-1R and PDGFR β in A431 cells, HEK-293. Cell progression 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. |
Cell Line: | MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells MT450, 1AS, ASM, G, AT6.1, MTLN3, MTLY, NM-081 cells |
Concentration: | 2.5, 10 μM 2.5, 10 μM |
Incubation Time: | 24 hours 24 hours |
Result: | Induced apoptosis in a wide variety of tumor cells. Blocked proliferation in a wide variety of tumor cells. Significantly suppressed the growth of MT450 tumors. |
in vivo studies | MAZ51 (8 mg/kg; I. p.; daily for 15 days) significant definitions the growth of MT450 tumors. Animal Model: Wistar Furth rats (bearing MT450 cells) Dosage: 8 mg/kg Administration: intraperone injection. |
Animal Model: | Wistar Furth rats (bearing MT450 cells) |
Dosage: | 8 mg/kg |
Administration: | Intraperitoneal injection; daily for 15 day |