1. Protein Tyrosine Kinase/RTK
  2. Anaplastic lymphoma kinase (ALK)
  3. CEP-28122

CEP-28122是一种高度有效的选择性ALK抑制剂, IC50值为1.9 ± 0.5 nM。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 CEP-28122 mesylate salt 通常具有更好的水溶性和稳定性。

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CEP-28122 Chemical Structure

CEP-28122 Chemical Structure

CAS No. : 1022958-60-6

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CEP-28122 的其他形式现货产品:

Customer Review

Other Forms of CEP-28122:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay. IC50 value: 1.9 ± 0.5 nM Target: ALK in vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells. [1] in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1]

分子量

539.07

Formula

C28H35ClN6O3

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
  • 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.

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产品名称:
CEP-28122
目录号:
HY-18030
需求量: