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  3. PPI-2458

PPI-2458 是一种口服有效的、选择性和不可逆的蛋氨酸氨基肽酶-2 (MetAP-2) 抑制剂。PPI-2458 可用于关节炎和淋巴瘤研究。

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PPI-2458 Chemical Structure

PPI-2458 Chemical Structure

CAS No. : 431077-35-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research[1][2].

体外研究
(In Vitro)

PPI-2458 可有效抑制 HUVEC 增殖,GI50 为0.2 nM,在1 nM 时最大抑制率大于 95%[1]
PPI-2458 (0-100 nM, 6天)抑制 SU-DHL-16 细胞的增殖和MetAP-2[2]

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

Cell Proliferation Assay[2]

Cell Line: SU-DHL-16 cells
Concentration: 0, 0.01, 0.1, 1, 10, and 100 nM
Incubation Time: 6 days
Result: Inhibited SU-DHL-16 proliferation in a dose-dependent fashion with maximum inhibition of 60% achieved at the highest concentration (100 nmol/L) and GI50 at 1.9 nmol/L.
体内研究
(In Vivo)

PPI-2458 (0-50 mg/kg,口服,隔日一次)逆转 PG-PS (25 mg/kg, i.p) 诱导的关节炎模型中的关节肿胀和炎症[1]
PPI-2458 (0-3 mg/kg,鼻胃插管,隔日一次)可导致实验初代食蟹猴生发中心生发中心淋巴细胞减少[2]
PPI-2458 (0-100 mg/kg,口服,隔日一次)以剂量依赖的方式显著抑制肿瘤生长在SR肿瘤异种移植的严重联合免疫缺陷小鼠中[2]

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

Animal Model: Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)[1]
Dosage: 0.25, 1, 5, and 50 mg/kg
Administration: Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
Result: Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.
Animal Model: Forty-two experimentally naive cynomolgus monkeys[2]
Dosage: 0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
Administration: Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
Result: Exhibited a marked decrease in germinal center lymphocytes.
Animal Model: 60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)[2]
Dosage: 10, 30, or 100 mg/kg
Administration: oral gavage, QOD
Result: Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.
Clinical Trial
分子量

424.53

Formula

C22H36N2O6

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

PPI-2458 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.

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