2. Metabolic Enzyme/Protease
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  4. A-357300

A-357300 是一种可逆且选择性的 MetAP2 抑制剂，对 MetAP2 和 MetAP1 的 IC50 值分别为 0.12 μM 和 57 μM。A-357300 可选择性地使内皮细胞和部分肿瘤细胞的细胞周期阻滞于 G1 期，从而诱导细胞增殖。A-357300 在体外和体内均能抑制血管生成，并在癌、肉瘤和神经母细胞瘤小鼠模型中显示出强大的抗肿瘤活性。A-357300 可用于神经母细胞瘤、纤维肉瘤和乳腺癌的研究。

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A-357300

A-357300 Chemical Structure

CAS No. : 369358-07-6

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A-357300 相关抗体

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MetAP2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

A-357300 (0.1 nM-100 μM, 3 d) 对内皮细胞和肿瘤细胞表现出选择性抗增殖活性，IC50 为 0.1-2 μM，但对人原代细胞几乎无此活性[1]。
A-357300 (10 μM, 3 d) 可诱导 HMVEC 或 HT-1080 细胞发生 G1 期细胞周期阻滞，从而导致细胞增殖停滞[1]。
A-357300 (0-10 μM, 1 d) 可降低 HMVEC 细胞中细胞周期蛋白 A 的浓度，同时保持细胞周期蛋白 D1 的浓度不变[1]。
A-357300 (0.08-2 μM, 3 d) 在 HMVEC 细胞中 0.4 μM 浓度下完全阻断管腔形成[1]。

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

A-357300 相关抗体:

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.
体内研究
(In Vivo)

A-357300 (25-100 mg/kg，皮下注射，每日两次，持续 7 天) 可抑制小鼠角膜血管生成[1]。
A-357300 (8-100 mg/kg，皮下注射，隔日一次或每日两次，持续 14-24 天) 可抑制小鼠神经母细胞瘤、纤维肉瘤和乳腺癌的生长[1]。

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.
分子量

359.87

Formula

C15H22ClN3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

A-357300 相关分类

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  • 稀释计算器

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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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