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Merck
CN

5.04173

MAT2A抑制剂II,FIDAS-5

别名:

MAT2A抑制剂II,FIDAS-5, 甲硫氨酸S-腺苷转移酶2A抑制剂II,FIDAS5,(E)-4-(2-氯-6-氟苯乙烯基)-N-甲基苯胺

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关于此项目

经验公式(希尔记法):
C15H13ClFN
化学文摘社编号:
分子量:
261.72
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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InChI key

KXVXICBOMOGFMH-JXMROGBWSA-N

SMILES string

Fc1c(c(ccc1)Cl)\C=C\c2ccc(cc2)NC

assay

≥98% (HPLC)

form

semisolid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 100 mg/mL

Quality Level

General description

细胞可渗透的FIDAS-3的氟化N,N-二烷基氨基均二苯乙烯(FIDAS)类似物,在无细胞测定(FIDAS-5的IC50 = 2.1 µM,FIDAS-3的IC50=4.9 µM;[L-Met]=[ATP]=1 mM,[MAT2A]=10 µg/mL;在反应30分钟之前预孵育FIDAS 20分钟)和基于细胞的(使用3 µM FIDAS-5或10µ M FIDAS-3处理36小时后,LS174T细胞中SAM和SAH水平分别降低64%和56%)测定中在抑制MAT2A催化的SAM(S-腺苷甲硫氨酸)合成方面均比FIDAS-3强>2倍。显示3 µM的FIDAS-5在体外可完全抑制LS174T CRC(结肠直肠癌)的增殖长达7 d,口服给药时,可有效抑制小鼠体内HT29 CRC肿瘤的扩增(在HT29异种移植18天后降低58%;从第4天开始20 mg/kg/天)。计算机辅助的计算机模拟预测FIDAS-3&-5在MAT2A二聚体的界面处靶向SAM结合口袋,并且体外结合研究显示FIDAS-3有效地与SAM竞争结合MAT2A。

Biochem/physiol Actions

主要靶标
MAT2A
可逆性:是
细胞可渗透性:具有

Packaging

用惰性气体包装

Preparation Note

复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多3个月。

Other Notes

Zhang, W., et al. 2013.ACS Chem. Biol.8, 796.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性:标准处理(A)

存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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