163655-37-6
中文名稱
CS-2885
英文名稱
MAZ51
CAS
163655-37-6
分子式
C21H18N2O
分子量
314.38
MOL 文件
163655-37-6.mol
更新日期
2024/11/05 14:06:53
163655-37-6 結(jié)構式
基本信息
中文別名
化合物MAZ513-((4-(二甲基氨基)萘-1-基)亞甲基)吲哚啉-2-酮
英文別名
MAZ51CS-2885
MAZ51
MAZ-51
MAZ 51
VEGFR3 Kinase Inhibitor, MAZ
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
2H-Indol-2-one, 3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-
安全數(shù)據(jù)
常見問題列表
生物活性
MAZ51 是一種選擇性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制劑。MAZ51 通過 Akt/GSK3β 的磷酸化和 RhoA 的激活來誘導神經(jīng)膠質(zhì)瘤細胞的細胞圓縮和G2/M細胞周期停滯。 MAZ51 可抑制多種非VEGFR-3表達腫瘤細胞的增殖并誘導其凋亡。靶點
| Target | Value |
|
VEGFR-3
() | |
|
Akt
() | |
|
GSK3β
() | |
|
RhoA
() |
體外研究
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. |
體內(nèi)研究
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. |