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392721-37-8

中文名稱(chēng) N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
英文名稱(chēng) N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
CAS 392721-37-8
分子式 C11H9ClF3NO2
分子量 279.64
MOL 文件 392721-37-8.mol
更新日期 2024/04/08 11:57:26
392721-37-8 結(jié)構(gòu)式 392721-37-8 結(jié)構(gòu)式

基本信息

中文別名
化合物FASENTIN
N-(4-氯-3-(三氟甲基)苯基)-3-氧代丁酰胺
英文別名
Fasentin
Fasentin NEW
Fasentin >=98% (HPLC)
Fasentin - CAS 392721-37-8 - Calbiochem
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide

物理化學(xué)性質(zhì)

儲(chǔ)存條件room temp
溶解度二甲基亞砜:>10mg/mL
形態(tài)粉末
顏色白色至灰白色
穩(wěn)定性DMSO中的溶液可在-20°下穩(wěn)定儲(chǔ)存3個(gè)月。

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類(lèi)別碼22
WGK Germany3
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-101849N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
Fasentin
392721-37-85mg700元
2024/11/08HY-101849N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
Fasentin
392721-37-810mM * 1mLin DMSO770元
2024/11/08HY-101849N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
Fasentin
392721-37-810mg1100元

常見(jiàn)問(wèn)題列表

生物活性
Fasentin 是有效的葡萄糖攝取抑制劑,可抑制 GLUT-1/GLUT-4 轉(zhuǎn)運(yùn)蛋白。Fasentin 優(yōu)先抑制 GLUT4 (IC50=68 μM)。Fasentin 是死亡受體刺激 (FAS) 敏化劑,可敏化細(xì)胞對(duì) FAS 誘導(dǎo)的細(xì)胞死亡。Fasentin 也是誘導(dǎo)腫瘤壞死因子 (TNF) 凋亡配體的敏化劑。Fasentin 阻斷癌細(xì)胞系中的葡萄糖攝取,并具有抗血管生成活性。
靶點(diǎn)

GLUT4

68 μM (IC 50 )

GLUT1

體外研究

Fasentin (0.1-1000 μM; 72?hours) inhibits endothelial, tumour and fibroblast cell growth without inducing cell death.
Fasentin (25-100 μM; 16-24 hours) induces a cell cycle arrest in G0/G1 phase and reduces the cell number in S phase in a dose-dependent manner.
Fasentin (50 μM; 16 hours) alters expression of genes associated with glucose deprivation such as AspSyn and PCK-2.
Fasentin (15, 30, 80 μM; pretreatment 1 hour) induces glucose deprivation, partially blocks glucose uptake in PPC-1, DU145, and U937 cells.
Fasentin (100 μM; 16 hours) does not affect the migratory capability of endothelial cells.
Fasentin (25-100 μM; 16?hours) lowers levels of phospho-ERK in HMECs, indicating a partial inhibition on the ERK signalling pathway, even though the effect is not statistically significant. Fasentin does not inhibit the tyrosine kinase activity of VEGFR2.
Fasentin interacts with a unique site in the intracellular channel of GLUT1.

Cell Viability Assay

Cell Line: Three types of endothelial cells ECs (HMEC, human microvascular endothelial cells; HUVEC, human umbilical vein endothelial cells; and BAEC, bovine aortic endothelial cells), three human tumour cell lines (MDA-MB-231 and MCF7 breast carcinoma cells, and HeLa cervix adenocarcinoma cells), and human gingival fibroblasts (HGF)
Concentration: 0.1, 1, 10, 100, 1000 μM
Incubation Time: 72?hours
Result: Inhibited endothelial, tumour and fibroblast cell growth (IC 50 =26.3-111.2 μM) without inducing cell death.

Cell Cycle Analysis

Cell Line: HMECs
Concentration: 25, 50, 100 μM
Incubation Time: 16, 24 hours
Result: Induced a cell cycle arrest in G0/G1 phase and reduced the cell number in S phase in a dose-dependent manner.
Did not increase the subG1 population.

RT-PCR

Cell Line: PPC-1 cells [2]
Concentration: 50 μM
Incubation Time: 16 hours
Result: Altered expression of genes associated with glucose deprivation such as AspSyn and PCK-2 not FLIP mRNA expression.
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