2. Apoptosis
  3. MDM-2/p53
  4. p53 Activator 15

p53 Activator 15 是一种口服有效的 p53 Y220C 激活剂。p53 Activator 15 增强 p53 Y220C 与 DNA 的结合能力 (SC50 = 0.58 nM)，显著抑制 NUGC-3 细胞增殖。p53 Activator 15 可有效抑制 NUGC-3 异种移植小鼠和大鼠模型中的肿瘤生长。p53 Activator 15 可用于研究胃癌。

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p53 Activator 15

p53 Activator 15 Chemical Structure

CAS No. : 3069395-29-2

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p53 Activator 15 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

p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer[1].

体外研究
(In Vitro)

p53 Activator 15 (Compound 2) 显著抑制 NUGC-3 细胞增殖，IC50 为 58 nM[1]。
p53 Activator 15 对 CYP 系列酶和 hERG 的抑制活性相对较弱或无显著差异，在人/大鼠/小鼠肝微粒体中也表现出较高的代谢稳定性[1]。

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

p53 Activator 15 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. CL 15 mL/min/kg
Mice 10 mg/kg p.o. Cmax 5.9 μM
Mice 1 mg/kg i.v. AUC0-t 1.7 μM·h
Mice 10 mg/kg p.o. AUC0-t 15.7 μM·h
体内研究
(In Vivo)

p53 Activator 15 (6.25-100 mg/kg，口服，每日一次，持续 19-28 天) 对小鼠和大鼠中 NUGC-3 移植肿瘤的增殖表现出优异的抑制活性[1]。

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

Animal Model: NUGC-3 transplanted tumors model established in female NuNu mice (6-8 weeks)[1]
Dosage: 25, 50 and 100 mg/kg
Administration: Oral administration (p.o.), once daily for 19 days
Result: Demonstrated good inhibitory activity against the proliferation of NUGC-3 transplanted tumors in mice at all tested doses, and exhibited dose-related properties.
Animal Model: NUGC-3 transplanted tumors model established in 7-9 week-old female B-Rag2/IL2rg knockout SD rats[1]
Dosage: 6.25, 12.5 and 25 mg/kg
Administration: Oral administration (p.o.), once daily for 28 days
Result: Demonstrated good inhibitory activity against the proliferation of NUGC-3 transplanted tumors in rats at all tested doses, and exhibited dose-related properties.
分子量

613.64

Formula

C27H27D3F4N6O4S
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

p53 Activator 15 相关分类

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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:

p53 Activator 153069395-29-2MDM-2/p53Activatorp53Y220CDNAAnti-cancerNUGC-3 xenograft mice modelHEK293 cellsNUGC-3 cellsBreast cancerStomach cancerLung cancerInhibitorinhibitorinhibit

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