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编 号：F754617
分子式：C19H16Cl2N2O3
分子量：391.25
分子式：C19H16Cl2N2O3
分子量：391.25
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CAS No: 2687265-18-3
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生物活性：
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer.
体内研究：
Anticancer agent 42 (compound 10d) (Kunming mice, 5000 mg/kg, Intragastric administration, once) has extremely low oral toxicity. Anticancer agent 42 (Kunming mice, 238-600 mg/kg, IP, once) shows no obvious liver and kidney damage to mice, with an LD50 of 374 mg/kg. Anticancer agent 42 (Kunming mice, 25 mg/kg, IP, once every two days) causes mild liver and kidney damage. Anticancer agent 42 (BALB/c mice, suppresses breast cancer 4T1 tumor growth, the anti-tumor effect is better combined use with CA (Cyanoacrylates), and can cross through the skin to achieve anti-tumor effects..Animal Model:Kunming mice (n=10, 5 male and 5 female)
Dosage:5000 mg/kg
Administration:Intragastric administration, once
Result:Had extremely low oral toxicity, did not cause death in mice at 5000 mg/kg.
Animal Model:Kunming mice
Dosage:600, 476, 378, 300, 238 mg/kg
Administration:IP, once
Result:Showed no obvious liver and kidney damage to mice, with an LD50 of 374 mg/kg.
Animal Model:Kunming mice (n=3)
Dosage:25 mg/kg
Administration:IP, once every two days
Result:Caused mild liver and kidney damage after administration, slightly increased ALT, AST and BUN of mice.
Animal Model:BALB/c mice (4T1 tumor-bearing, female, eight groups, 6 mice per group)
Dosage:10d (50 mg/kg) + CA; 10d (50 mg/kg) + saline; 10d (200 mg/kg) + CA
Administration:Intratumoral injection, every four days (50 mg/kg); smear, every two days (200 mg/kg), for 14 days.
Result:Showed obvious antitumor effect from the 8th day; had protective effects on the spleens of tumor-bearing mice; the anti-tumor effect is better when combined use with CA; can cross through the skin to achieve anti-tumor effects.
体外研究：
Anticancer agent 42 (compound 10d) (0-20 μM, 4 h) exhibits a potent antitumor activity against MDA-MB-231 cells.Anticancer agent 42 (10 μM, 24 h) induces G2 and S phase arrest in MDA-MB-231 cells.Anticancer agent 42 (10 μM, 24 h) induces cell apoptosis by regulating the expression of apoptosis related proteins in MDA-MB-231 cells.Anticancer agent 42 (0-1 μM) depolarizes mitochondrial membrane and decreases the mitochondrial membrane potential leading to apoptosis.Anticancer agent 42 (0-1 μM, 24 h) induces the cells to produce a large amount of ROS.
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer.
体内研究：
Anticancer agent 42 (compound 10d) (Kunming mice, 5000 mg/kg, Intragastric administration, once) has extremely low oral toxicity. Anticancer agent 42 (Kunming mice, 238-600 mg/kg, IP, once) shows no obvious liver and kidney damage to mice, with an LD50 of 374 mg/kg. Anticancer agent 42 (Kunming mice, 25 mg/kg, IP, once every two days) causes mild liver and kidney damage. Anticancer agent 42 (BALB/c mice, suppresses breast cancer 4T1 tumor growth, the anti-tumor effect is better combined use with CA (Cyanoacrylates), and can cross through the skin to achieve anti-tumor effects..Animal Model:Kunming mice (n=10, 5 male and 5 female)
Dosage:5000 mg/kg
Administration:Intragastric administration, once
Result:Had extremely low oral toxicity, did not cause death in mice at 5000 mg/kg.
Animal Model:Kunming mice
Dosage:600, 476, 378, 300, 238 mg/kg
Administration:IP, once
Result:Showed no obvious liver and kidney damage to mice, with an LD50 of 374 mg/kg.
Animal Model:Kunming mice (n=3)
Dosage:25 mg/kg
Administration:IP, once every two days
Result:Caused mild liver and kidney damage after administration, slightly increased ALT, AST and BUN of mice.
Animal Model:BALB/c mice (4T1 tumor-bearing, female, eight groups, 6 mice per group)
Dosage:10d (50 mg/kg) + CA; 10d (50 mg/kg) + saline; 10d (200 mg/kg) + CA
Administration:Intratumoral injection, every four days (50 mg/kg); smear, every two days (200 mg/kg), for 14 days.
Result:Showed obvious antitumor effect from the 8th day; had protective effects on the spleens of tumor-bearing mice; the anti-tumor effect is better when combined use with CA; can cross through the skin to achieve anti-tumor effects.
体外研究：
Anticancer agent 42 (compound 10d) (0-20 μM, 4 h) exhibits a potent antitumor activity against MDA-MB-231 cells.Anticancer agent 42 (10 μM, 24 h) induces G2 and S phase arrest in MDA-MB-231 cells.Anticancer agent 42 (10 μM, 24 h) induces cell apoptosis by regulating the expression of apoptosis related proteins in MDA-MB-231 cells.Anticancer agent 42 (0-1 μM) depolarizes mitochondrial membrane and decreases the mitochondrial membrane potential leading to apoptosis.Anticancer agent 42 (0-1 μM, 24 h) induces the cells to produce a large amount of ROS.
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