CA-5F

生物活性靶点体外研究体内研究 CA-5F 试剂级价格

CA-5F

CAS号:1370032-19-1
英文名:CA-5f
中文名:CA-5F
CBNumber:CB04808619
分子式:C24H24N2O3
分子量:388.46
MOL File:1370032-19-1.mol

CA-5F化学性质

沸点 :639.7±55.0 °C(Predicted)
密度 :1.253±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO : 77.5 mg/mL (199.51 mM);Water : < 0.1 mg/mL (insoluble)
酸度系数(pKa) :16.06±0.30(Predicted)
形态 :Solid
颜色 :Light yellow to yellow

CA-5F性质、用途与生产工艺

生物活性 CA-5f 是一种有效的晚期巨自噬/自噬 (macroautophagy/autophagy) 抑制剂，通过抑制自噬体-溶酶体融合起作用。CA-5f 能够增加 LC3B-II (一种监控自噬的标记物) 和 SQSTM1 蛋白水平，促进 ROS 的产生。具有抗肿瘤活性。
靶点

Macroautophagy/autophagy

体外研究

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.

体内研究

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.