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CAY10681 (Synonyms:p53-MDM2-IN-2)
目录号 : KCM11636 CAS No. : 1542066-69-2 纯度 : ≥98%
Data Sheet 产品使用指南
Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (K = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (ICs range from 33 to 37 µM). CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.
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5mg
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25mg
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生物活性

CAY10681 is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. CAY10681 exerts antitumor activity by inhibiting NF-κB pathway.
体外研究

CAY10681 (0.1-20 μM, 4 h) dose-dependently increased p65 levels in the cytoplasm and nucleus of A549 cells.
体内研究

CAY10681 (200 mg/kg, gavage, 14 days) effectively inhibited tumor growth in A549 xenograft model.
分子式
C30H26BrN5O
分子量
552.46
CAS号
1542066-69-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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