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编 号：F762988
分子式：C16H20Cl2N2O4Pt
分子量：570.33
分子式：C16H20Cl2N2O4Pt
分子量：570.33
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CAS No: 3032101-64-4
产品详情
生物活性：
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
体内研究：
Antitumor agent-37 (compound 7) (i.p.; 4 mg Pt/kg; four times on days 3, 6, 9, and 12 post-tumor inoculation) exerts no visible impacts on body weight of mice in comparison with the blank group, which is obviously superior to reference drug OLP and complex 9, indicating its low toxicity in vivo.Antitumor agent-37 (compound 7) (i.p.; 4 mg Pt/kg; four times on days 3, 6, 9, and 12 post-tumor inoculation) also exhibits prominent tumor growth inhibition to 4T1 tumors with a TGI of 54.6%.Antitumor agent-37 (compound 7) (i.p.; 2 mg Pt/kg; four times on days 2, 4, 6, 8, 10, 12, and 14 post-tumor inoculation) displays significantly more effective antimetastasis effects than CDDP and OLP in vivo.Animal Model:Male BALB/c mice bearing CT-26 homograft tumors(18-20 g); female BALB/C mice bearing murine 4T1 cells (18–20 g)
Dosage:4 mg Pt/kg
Administration:i.p.; four times on days 3, 6, 9, and 12 post-tumor inoculation
Result:Exerted no visible impacts on body weight of mice in comparison with the blank group, which was obviously superior to reference drug OLP and complex 9, indicating its low toxicity in vivo. Antitumor agent-37 also exhibited prominent tumor growth inhibition to 4T1 tumors with a TGI of 54.6%.
Animal Model:BALB/C mice bearing murine 4T1 cells
Dosage:2 mg Pt/kg
Administration:i.p.; four times on days 2, 4, 6, 8, 10, 12, and 14 post-tumor inoculation
Result:Decreased metastatic nodules examined by H&E staining in the lung and obviously smaller than that from the blank group as well as CDDP and OLP groups.
体外研究：
Antitumor agent-37 (compound 7) (24-76 hours) displays relatively lower activities after 24 h treatment, and the IC50 values decreases at 48 h, and the activities at 72 h are similar to that of 48 h.Antitumor agent-37 (compound 7) (24 hours) induces significant apoptosis of tumor cells in a dose-dependent manner.Antitumor agent-37 (compound 7) (24 hours) induces serious apoptosis of tumor cells by the activation of mitochondrial pathway Bcl-2/Bax/caspase3.
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
体内研究：
Antitumor agent-37 (compound 7) (i.p.; 4 mg Pt/kg; four times on days 3, 6, 9, and 12 post-tumor inoculation) exerts no visible impacts on body weight of mice in comparison with the blank group, which is obviously superior to reference drug OLP and complex 9, indicating its low toxicity in vivo.Antitumor agent-37 (compound 7) (i.p.; 4 mg Pt/kg; four times on days 3, 6, 9, and 12 post-tumor inoculation) also exhibits prominent tumor growth inhibition to 4T1 tumors with a TGI of 54.6%.Antitumor agent-37 (compound 7) (i.p.; 2 mg Pt/kg; four times on days 2, 4, 6, 8, 10, 12, and 14 post-tumor inoculation) displays significantly more effective antimetastasis effects than CDDP and OLP in vivo.Animal Model:Male BALB/c mice bearing CT-26 homograft tumors(18-20 g); female BALB/C mice bearing murine 4T1 cells (18–20 g)
Dosage:4 mg Pt/kg
Administration:i.p.; four times on days 3, 6, 9, and 12 post-tumor inoculation
Result:Exerted no visible impacts on body weight of mice in comparison with the blank group, which was obviously superior to reference drug OLP and complex 9, indicating its low toxicity in vivo. Antitumor agent-37 also exhibited prominent tumor growth inhibition to 4T1 tumors with a TGI of 54.6%.
Animal Model:BALB/C mice bearing murine 4T1 cells
Dosage:2 mg Pt/kg
Administration:i.p.; four times on days 2, 4, 6, 8, 10, 12, and 14 post-tumor inoculation
Result:Decreased metastatic nodules examined by H&E staining in the lung and obviously smaller than that from the blank group as well as CDDP and OLP groups.
体外研究：
Antitumor agent-37 (compound 7) (24-76 hours) displays relatively lower activities after 24 h treatment, and the IC50 values decreases at 48 h, and the activities at 72 h are similar to that of 48 h.Antitumor agent-37 (compound 7) (24 hours) induces significant apoptosis of tumor cells in a dose-dependent manner.Antitumor agent-37 (compound 7) (24 hours) induces serious apoptosis of tumor cells by the activation of mitochondrial pathway Bcl-2/Bax/caspase3.
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