| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C15H22ClN3O3S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
A-357300 is a reversible, selective inhibitor of MetAP2, with IC50 values of 0.12 μM and 57 μM against MetAP2 and MetAP1, respectively. It induces cytostasis through G1-phase cell cycle arrest selectively in endothelial cells and in a subset of tumor cells, inhibits angiogenesis both in vitro and in vivo, and shows potent antitumor efficacy in carcinoma, sarcoma, and neuroblastoma murine models. It can be used for studies of neuroblastoma, fibrosarcoma, and breast cancer[1]. It has a molecular formula of C15H22ClN3O3S and a molecular weight of 359.87 g/mol.
Physical & Chemical Properties
| CAS Number | 369358-07-6 |
|---|---|
| Molecular Formula | C15H22ClN3O3S |
| Molecular Weight | 359.87 g/mol |
| SMILES | CC(C)SCC[C@@H](N)[C@H](O)C(NNC(C1=CC(Cl)=CC=C1)=O)=O |
| Target | MetAp2, MetAp1 |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
MetAp2 0.12 μM (IC50) |
MetAp1 57 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Endothelial cells and tumor cells are targeted by A-357300 (0.1 nM-100 μM, 3 days) with selective antiproliferative activity, showing IC50s of 0.1-2 μM, but human primary cells are not affected[1]. In HMVECs or HT-1080 cells, A-357300 (10 μM, 3 days) induces cytostasis through cell cycle arrest at the G1 phase[1]. In HMVECs, A-357300 (0-10 μM, 1 day) lowers cyclin A concentration while cyclin D1 concentration stays unchanged[1]. Lumen formation in HMVECs is completely blocked at 0.4 μM by A-357300 (0.08-2 μM, 3 days)[1].
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
Mouse cornea angiogenesis is inhibited by A-357300 (25-100 mg/kg, s.c., twice daily for 7 days)[1]. The growth of neuroblastoma, fibrosarcoma and breast cancer in mice is inhibited by A-357300 (8-100 mg/kg, s.c.; dosed twice daily or once every other day, for 14-24 days)[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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