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  3. Antitumor agent-212

Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study.

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Antitumor agent-212

Antitumor agent-212 Chemical Structure

CAS No. : 3108305-08-1

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Description

Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study[1].

In Vitro

Antitumor agent-212 (compound 2d) (72 h) exhibits potent antiproliferative activity against U87 cells (IC50 = 0.87 μM), C6 cells (IC50 = 0.85 μM), 4T1 cells (IC50 = 0.95 μM) and A549 cells (IC50 = 1.32 μM), and shows high selectivity for cancer cells over normal HEK293T cells (IC50 = 77.15 μM)[1].
Antitumor agent-212 exhibits an MIC value of 128 μg/mL (302.6 μM) against Gram-positive Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA), and no activity against Gram-negative Pseudomonas aeruginosa (MIC > 256 μg/mL)[1].PARP1/NAMPT-IN-1 (0.3-1 μM; 48 h) enhances TBK1 and IRF3 phosphorylation in MDA-MB-231 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Antitumor agent-212 (compound 2d) (30 mg/kg; i.p. and S.C.; once a day; for 15 days) exerts significant tumor growth inhibition with no obvious toxicity in U87 human glioma xenograft models of male BALB/C nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/C nude mice were implanted with U87 human glioma cells to establish orthotopic xenograft models[1].
Dosage: 30 mg/kg
Administration: Intraperitoneal (IP) and subcutaneous (S.C.) injection; once daily; for 15 days
Result: Significantly inhibited tumor growth from day 12 and reduced tumor volume markedly on day 15 compared to the control group.
No obvious toxicity was observed in mice, with no body weight loss during the experimental period.
Molecular Weight

422.81

Formula

C20H22ClNO2Se

CAS No.
SMILES

CN(C)CC(CC(C[Se]C1=CC=CC=C1)(C2=CC=C(Cl)C=C2)O3)C3=O

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Antitumor agent-212
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HY-181517
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