2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.:163655-37-6 Product 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 EINEC: Molecular Formula:C21H18N2O Molecular Weight:314.38000
Target:
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.
Kinase Assay
Cell Assay
Animal Administration
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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