2. Metabolic Enzyme/Protease
  3. MetAP
  4. 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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A-357300

A-357300 Chemical Structure

CAS No. : 369358-07-6

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Description

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[1].

In Vitro

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.

A-357300 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HMVECs and HT-1080 cells
Concentration: 10 μM
Incubation Time: 3 days
Result: Showed G1 phase arrest, with no accumulation of sub-G1 phase cells.

Western Blot Analysis[1]

Cell Line: HMVECs
Concentration: 0, 0.001, 0.01, 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Reduced the concentration of cyclin A, while keeping the concentration of cyclin D1 unchanged.
In Vivo

A-357300 (25-100 mg/kg, s.c., twice daily for 7 days) shows inhibition of mouse cornea angiogenesis[1].
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.

Animal Model: Corneal angiogenesis model established in CF1 mice[1]
Dosage: 25, 75 and 100 mg/kg
Administration: Subcutaneous injection (s.c.), twice daily for 7 days
Result: Inhibited growth factor-induced cornea neovascularization in a dose-dependent manner against VEGF, and against bFGF.
Animal Model: CHP-134 neuroblastoma xenograft model established in mice[1]
Dosage: 100 mg/kg
Administration: Subcutaneous injection (s.c.), twice daily for 24 days
Result: Significantly suppressed growth of this established tumor xenograft with a T/C of 0.185 on day 24 after the initiation of treatment.
Animal Model: HT-1080 fibrosarcoma xenograft model established in SCID-beige mice[1]
Dosage: 15, 30, 60 and 100 mg/kg
Administration: Subcutaneous injection (s.c.), twice daily for 14-16 days
Result: Inhibited tumor growth in a dose-dependent manner and no overt signs of toxicity were observed.
Animal Model: MDA-435-LM breast cancer xenograft model established in SCID mice[1]
Dosage: 8, 16, 20 mg/kg (group 1); 50 and 100 mg/kg (group 2)
Administration: Subcutaneous injection (s.c.), once every other day (group 1) or twice daily (group 2) for 20 days
Result: Exhibited better efficacy in group 2 than group 1.
Molecular Weight

359.87

Formula

C15H22ClN3O3S
CAS No.
SMILES

CC(C)SCC[C@@H](N)[C@H](O)C(NNC(C1=CC(Cl)=CC=C1)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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A-357300 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-357300369358-07-6A357300A 357300MetAPMethionine AminopeptidaseTNP-470Cytostasis?Angiogenesis InhibitionEndothelial Cells (ECs)?Xenograft ModelsInhibitorinhibitorinhibit

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