2. Cell Cycle/DNA Damage Stem Cell/Wnt
  3. Casein Kinase
  4. APL-5125

APL-5125 (Compound 61f) 是一种强效、选择性且具有口服活性的 ATP 竞争性 CK2α 抑制剂，其 IC50 值为 0.348 nM，Ki 值为 0.095 nM。APL-5125 以双价方式与 CK2α 结合，同时与 ATP 结合位点和 αD 口袋相互作用。APL-5125 具有抗肿瘤活性，可用于癌症研究，如结直肠癌。

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APL-5125

APL-5125 Chemical Structure

CAS No. : 2830619-57-1

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APL-5125 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer[1].

IC50 & Target[1]

CK2α

0.348 nM (IC50)

CK2α

0.095 nM (Ki)

体内研究
(In Vivo)

APL-5125 (10-100 mg/kg；口服；每日一次；21 天) 在携带 HCT-116 细胞的小鼠中抑制肿瘤生长[1]。

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

Animal Model: Mice bearing with HCT-116 cells[1]
Dosage: 10, 30 and 100 mg/kg
Administration: Oral administration, once daily for 21 days
Result: Showed tumor-growth inhibition with 45% at 100 mg/kg.
分子量

565.49

Formula

C27H24F5N3O5
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

APL-5125 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 *
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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)
× = ×
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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:

APL-51252830619-57-1APL5125APL 5125Casein KinasetumorspreclinicalexposurePK-PDpotencyS129cellularselectivitykinaseHCT116profileCK2αp-AKTdruginhibitorunboundInhibitorinhibit

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产品名称：
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目录号：
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