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Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrial membrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research[1]. | [in vivo]
Antitumor agent-115 (SS-12) (10 mg stachydrine/kg equivale, 200 μL for Oral administration) has greater bioavailability in rats[1].
Antitumor agent-115 (0.2 mmol/kg for Oral administration) has anti-tumor effects in breast cancer model mice and improves morphological structure of spleen in model mice[1].
| Animal Model: | Rats[1] | | Dosage: | 10 mg stachydrine/kg equivale, 200 μL | | Administration: | Oral administration (p. o.) | | Result: | Exhibited high systemic exposure with 6.10 μg/mL of Cmax value and 14.75 h μg/mL of AUC0-t value. |
| Animal Model: | Tumor-bearing mice[1] | | Dosage: | 0.2 mmol/kg | | Administration: | Oral administration (p. o.) | | Result: | Inhibitory rate was 51.47% ( P < 0.01)
Displayed significant tumor cell shrinkage and larger void areas in tumor tissues
Exhibited more weight loss than the model group and other treatment groups, increased of both AST and ALT levels and reduced spleen index of the tumor-bearing mice
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| [References]
[1] Zeng H, et al. Synthesis, characterization and anti-breast cancer activities of stachydrine derivatives. Eur J Med Chem. 2023 Jul 26;259:115679. DOI:10.1016/j.ejmech.2023.115679 |
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