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1370032-19-1

中文名稱 CA-5F
英文名稱 CA-5f
CAS 1370032-19-1
分子式 C24H24N2O3
分子量 388.46
MOL 文件 1370032-19-1.mol
更新日期 2024/11/05 14:06:54
1370032-19-1 結(jié)構(gòu)式 1370032-19-1 結(jié)構(gòu)式

基本信息

中文別名
化合物CA-5F
英文別名
CA-5f
CA-5F
CA 5F
CA5F
1370032-19-1
-5-(1H-indol-3-ylmethylene)-1-methyl-, (3E,5E)-
4-Piperidinone, 3-[(3,4-dimethoxyphenyl)methylene]-5-(1H-indol-3-ylmethylene)-1-methyl-, (3E,5E)-

物理化學(xué)性質(zhì)

沸點(diǎn)639.7±55.0 °C(Predicted)
密度1.253±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 77.5 mg/mL (199.51 mM);Water : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)16.06±0.30(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

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-H315-H319-H335

常見問題列表

生物活性
CA-5f 是一種有效的晚期巨自噬/自噬 (macroautophagy/autophagy) 抑制劑,通過抑制自噬體-溶酶體融合起作用。CA-5f 能夠增加 LC3B-II (一種監(jiān)控自噬的標(biāo)記物) 和 SQSTM1 蛋白水平,促進(jìn) ROS 的產(chǎn)生。具有抗腫瘤活性。
靶點(diǎn)

Macroautophagy/autophagy

體外研究

CA-5f (0-40 μM, 6 hour) concentration- and time-dependently elevates the level of LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs.
CA-5f (20 μM, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combination Bafilomycin A1 (100 nM) or Chloroquine (30 μM) in A549 cells and HUVECs.
CA-5f (20 μM) neither impairs the hydrolytic function nor the quantity of lysosomes.
CA-5f (20 μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs.

Cell Viability Assay

Cell Line: A549, HUVECs
Concentration: 20 μM
Incubation Time: 96 hours
Result: Exhibited more cytotoxicity against A549 cells compared with normal HUVECs.

Western Blot Analysis

Cell Line: A549 cells and HUVECs
Concentration: 0-40 μM
Incubation Time: 6 hours
Result: Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in a concentration- and time-dependent manner.
體內(nèi)研究

CA-5f (40 mg/kg, i.p., every 2 days for up to 30 days) is well tolerated, and potently inhibits the growth of tumor in nude mice bearing A549 lung cancer cells.
CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells.

Animal Model: Nude mice bearing A549 lung cancer cells
Dosage: 40 mg/kg
Administration: Injected via caudal vein, every 2 days for up to 30 days
Result: Significantly suppressed tumor volume and weight in mice, increased the number of apoptotic cells in mice.
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