A-357300
A-357300 is a reversible and selective MetAP2 inhibitor with IC50s of 0.12 and 57 μM against MetAP2 and MetAP1. A-357300 induces cytostasis by cell cycle arrest at the G1 phase selectively in endothelial cells and in a subset of tumor cells. A-357300 inhibits angiogenesis both in vitro and in vivo and shows potent antitumor efficacy in carcinoma, sarcoma, and neuroblastoma murine models. A-357300 can be used for the studies of neuroblastoma, fibrosarcoma and breast cancer.
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- CAS No.: 369358-07-6
- Formule: C15H22ClN3O3S
- Masse moléculaire:359.87
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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MetAp2 0.12 μM (IC50) |
MetAp1 57 μM (IC50) |
A-357300 (0.1 nM-100 μM, 3 days) exhibits selective antiproliferative activity against endothelial cells and tumor cells with IC50s of 0.1-2 μM, but not in human primary cells[1].
A-357300 (10 μM, 3 days) induces cytostasis by cell cycle arrest at the G1 phase in HMVECs or HT-1080 cells[1].
A-357300 (0-10 μM, 1 day) reduces the concentration of cyclin A, while keeping the concentration of cyclin D1 unchanged in HMVECs[1].
A-357300 (0.08-2 μM, 3 days) completely blocks the formation of the lumen at a concentration of 0.4 μM in HMVECs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMVECs and HT-1080 cells
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Concentration:10 μM
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Incubation Time:3 days
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Result:Showed G1 phase arrest, with no accumulation of sub-G1 phase cells.
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Cell Line:HMVECs
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Concentration:0, 0.001, 0.01, 0.1, 1 and 10 μM
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Incubation Time:24 h
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Result:Reduced the concentration of cyclin A, while keeping the concentration of cyclin D1 unchanged.
A-357300 (8-100 mg/kg, s.c., once every other day or twice daily for 14-24 days) inhibits the growth of neuroblastoma, fibrosarcoma and breast cancer in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Corneal angiogenesis model established in CF1 mice[1]
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Dosage:25, 75 and 100 mg/kg
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Administration:Subcutaneous injection (s.c.), twice daily for 7 days
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Result:Inhibited growth factor-induced cornea neovascularization in a dose-dependent manner against VEGF, and against bFGF.
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Animal Model:CHP-134 neuroblastoma xenograft model established in mice[1]
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Dosage:100 mg/kg
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Administration:Subcutaneous injection (s.c.), twice daily for 24 days
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Result:Significantly suppressed growth of this established tumor xenograft with a T/C of 0.185 on day 24 after the initiation of treatment.
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Animal Model:HT-1080 fibrosarcoma xenograft model established in SCID-beige mice[1]
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Dosage:15, 30, 60 and 100 mg/kg
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Administration:Subcutaneous injection (s.c.), twice daily for 14-16 days
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Result:Inhibited tumor growth in a dose-dependent manner and no overt signs of toxicity were observed.
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Animal Model:MDA-435-LM breast cancer xenograft model established in SCID mice[1]
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Dosage:8, 16, 20 mg/kg (group 1); 50 and 100 mg/kg (group 2)
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Administration:Subcutaneous injection (s.c.), once every other day (group 1) or twice daily (group 2) for 20 days
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Result:Exhibited better efficacy in group 2 than group 1.
Chemical Information
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CAS No. 369358-07-6
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Masse moléculaire 359.87
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Formule C15H22ClN3O3S
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SMILES
CC(C)SCC[C@@H](N)[C@H](O)C(NNC(C1=CC(Cl)=CC=C1)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-357300 Related Classifications
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