Antitumor agent-37 具有有效的抗增殖和抗转移活性。Antitumor agent-37 诱导严重的 DNA 损伤并进一步导致 γ-H2AX 和 p53 的高表达。Antitumor agent-37通过线粒体Apoptosis" style="display: inline; color: #c13a36">凋亡通路 BCL-2/Bax/Caspase3 促进肿瘤细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。Antitumor agent-37 通过抑制 PD-L1 的表达以增加肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞显著改善免疫反应。

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 [1].

Antitumor agent-37 (compound 7) (24-76 hours) displays relatively lower activities after 24 h treatment, and the IC 50 values decreases at 48 h, and the activities at 72 h are similar to that of 48 h [1]. Antitumor agent-37 (compound 7) (24 hours) induces significant apoptosis of tumor cells in a dose-dependent manner [1]. Antitumor agent-37 (compound 7) (24 hours) induces serious apoptosis of tumor cells by the activation of mitochondrial pathway Bcl-2/Bax/caspase3 [1]. Apoptosis Analysis [1] Cell Line: murine tumor cell line 4T1 and human tumor cell line A549 Concentration: 5 and 10 μM Incubation Time: 24 hours Result: Exhibited effective apoptosis induction of both A549 and 4T1 cells after 24 h treatment. Western Blot Analysis [1] Cell Line: A549 cells Concentration: 10 μM Incubation Time: 24 hours Result: Dramatically downregulated the level of anti-apoptotic Bcl-2 and increased the secretion of pro-apoptotic Bax. Subsequently, the apoptosis executor caspase3 and c-caspase3 were remarkably upregulated by antitumor agent-37.

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 [1]. 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% [1]. 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 [1]. 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) [1] 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 [1] 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.

C16H18Cl2N2O4Pt

568.32

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years