MAZ51

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MAZ51 是一种 VEGFR-3 (Flt-4) 酪氨酸激酶抑制剂。 MAZ51 能够阻断表达 VEGFR-3 的人内皮细胞的增殖，并且诱导其凋亡的能力较弱。

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.

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 μMIncubation 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.

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 dayResult:Significantly suppressed the growth of MT450 tumors.

——

Angiogenesis

VEGFR

VEGFR3

——

——

163655-37-6

314.38

C21H18N2O

>98% (HPLC)

DMSO:3.33 mg/ml(10.59 mM; Need ultrasonic)

CN(C)c1ccc(C=C2C(=O)Nc3ccccc23)c2ccccc12

——

(-20℃)

With Ice Pack

≥ 2 years