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| Cas No.: | 163655-37-6 |
| Chemical Name: | MAZ51 |
| Synonyms: | 2H-Indol-2-one,3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-;MAZ51;3-(4-Dimethylaminonaphthalen-1-ylmethylene)-1,3-dihydroindol-2-one;3-(4-DIMETHYLAMINO-NAPHTHALEN-1-YLMETHYLENE)-1,3-DIHYDRO-INDOL-2-ONE;(3E)-3-[[4-(dimethylamino)naphthalen-1-yl]methylidene]-1H-indol-2-one;(3E)-3-{[4-(Dimethylamino)-1-naphthyl]methylene}-1,3-dihydro-2H-indol-2-one |
| SMILES: | CN(C1=CC=C(C2=CC=CC=C21)/C=C/3\C4=CC=CC=C4NC3=O)C |
| Formula: | C21H18N2O |
| M.Wt: | 314.38000 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity[1][2]. |
| In Vivo: | MAZ51 (8 mg/kg; i.p.; daily for 15 day) significantly suppresses the growth of MT450 tumors[2]. Animal Model: Wistar Furth rats (bearing MT450 cells)[1] 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[2]. 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[2]. Cell Proliferation Assay[2] 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[2] 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. |
| References: | [1]. Kirkin V, et al. Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2. Eur J Biochem. 2001 Nov;268(21):5530-40. [2]. Kirkin V, et al. MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo. Int J Cancer. 2004 Dec 20;112(6):986-93. |
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