2. Metabolic Enzyme/Protease
  3. Proteasome
  4. Anticancer agent 114

Anticancer agent 114 是一种口服有效的二肽硼酸酯蛋白酶体抑制剂，IC50 值为 2.2 nM。Anticancer agent 114 对 RPMI-8226 细胞具有抗增殖活性。Anticancer agent 114 可用于多发性骨髓瘤的研究。

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Anticancer agent 114 Chemical Structure

Anticancer agent 114 Chemical Structure

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Anticancer agent 114 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 114 is a potent and orally active dipeptide boronic acid ester proteasome inhibitor with an IC50 value of 2.2 nM. Anticancer agent 114 has antiproliferative activity against the RPMI-8226 cells. Anticancer agent 114 can be used in research of multiple myeloma[1].

体外研究
(In Vitro)

Anticancer agent 114 (compound 18u; 0-2 μM; 24 h) 对 RPMI-8226 细胞具有抗增殖活性，IC50 值为 5.6 nM[1]。

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

Anticancer agent 114 相关抗体:

Cell Viability Assay[1]

Cell Line: RPMI-8226 cells
Concentration: 0-2 μM
Incubation Time: 24 hours
Result: Inhibited cell growth in a dose-dependent manner.
体内研究
(In Vivo)

Anticancer agent 114 (compound 18u; 6 and 10 mg/kg; p.o.; 每周两次, 持续 21 天) 在人 MM (RPMI-8226) 异种移植小鼠模型中表现出抗癌功效[1]。
Anticancer agent 114 (0.4 mg/kg and 1.2 mg/kg; i.v and p.o.; 雄性 Sprague-Dawley 大鼠) 表现出良好的微粒体稳定性和药代动力学特性[1]。

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

Animal Model: Female Balb/c nude mice with human MM (RPMI-8226) xenografts[1]
Dosage: 6 and 10 mg/kg
Administration: oral administration; twice a week, for 21 days
Result: Inhibited tumor growth in a dose-dependent manner.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 0.4 mg/kg and 1.2 mg/kg
Administration: 0.4 mg/kg (i.v.) and 1.2 mg/kg (p.o.)
Result: 1.19
Dose i.v. (0.4 mg/kg) i.g. (1.2 mg/kg)
Cmax (ng/mL) - 174
Tmax (h) - 0.83
T1/2 (h) 24.14 30
Cls 0.44 -
AUC0-t (ng·h/mL) 2270 2680
F % - 34
分子量

634.37

Formula

C28H33BF6N2O7
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

Anticancer agent 114 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

Anticancer agent 114Anticancer agent114Anticancer agent-114Proteasomedipeptide boronic acid esterantiproliferativeRPMI-8226 cellsmultiple myelomaInhibitorinhibitorinhibit

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