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Antitumor agent-51 

Cat. No.: HY-115996
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Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity.

For research use only. We do not sell to patients.

Antitumor agent-51 Chemical Structure

Antitumor agent-51 Chemical Structure

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Description

Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity[1].

IC50 & Target

IC50: 21.9 nM in MNNG/HOS cells[1]

In Vitro

Antitumor agent-51 (compound R-8i) (0-20 μM; 72 hours) selectively inhibits MNNG/HOS OS cells proliferation with IC50=21.9 nM, and has much less inhibitory activity on two normal BMSC and GES1 cells (IC50>10 μM)[1].
Antitumor agent-51 (5 nM; 24 hours) induces a cell cycle arrest in MNNG/HOS cells with a 23% increase in G0/G1 phase, but no apparent cell apoptosis[1].
Antitumor agent-51 (5 and 20 nM; 24 hours) significantly suppresses the migration of MNNG/HOS cells[1].

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

Cell Proliferation Assay

Cell Line: MNNG/HOS, MG63, SJSA-1, U2OS, 143B, SAOS-2, HOS, SW1353, GES1, and BMSC cells[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Selectively inhibited MNNG/HOS cells proliferation with IC50=21.9 nM, and showed much less inhibitory activity on two normal BMSC and GES1 cells (IC50>10 μM).

Cell Cycle Analysis

Cell Line: MNNG/HOS cells[1]
Concentration: 5 nM
Incubation Time: 24 hours
Result: Induced a cell cycle arrest with a 23% increase in G0/G1 phase, but no apparent cell apoptosis.
In Vivo

Antitumor agent-51 (12.5 or 62.5 mg/kg; i.p. or i.v., single) exhibits good intraperitoneal plasma exposures (AUC0-∞>6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration in male ICR mice[1].
Antitumor agent-51 (62.5 mg/kg; i.p., twice per day for 18 days) significantly suppresses MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and does not induce an obvious toxicity in nude mice[1].
Pharmacokinetic Parameters of Antitumor agent-51 in male ICR mice[1].

IV (12.5 mg/kg) IP (62.5 mg/kg)
T1/2 (h) 0.061 0.641
AUC0-inf (h·ng/mL) 3230 8406
Cmax (ng/mL) 20511
CL (mL/min/kg) 66.9
F (%) 52.1

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

Animal Model: Male ICR mice (30 g, n=3)[1]
Dosage: 12.5 or 62.5 mg/kg
Administration: i.p. or i.v., single (Pharmacokinetic Analysis)
Result: Showed good intraperitoneal plasma exposures (AUC0-∞ > 6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration.
Animal Model: Female BALB/c nude mice (3 months, human MNNG/HOS xenografts)[1]
Dosage: 62.5 mg/kg
Administration: i.p., twice per day for 18 days
Result: Significantly suppressed MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and did not induce an obvious toxicity.
Molecular Weight

435.54

Formula

C23H25N5O2S

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Antitumor agent-51
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HY-115996
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