1. Apoptosis JAK/STAT Signaling
  2. PKD Pim Apoptosis
  3. CRT0066101

CRT0066101 是一种有效的具有口服活性的 PKD 抑制剂,对 PKD1PKD2PKD3IC50 值分别为 1 nM、2.5 nM 和 2 nM。CRT0066101 也是一种有效的 PIM2 抑制剂,IC50 约为 135.7nM。CRT0066101 具有抗癌作用。

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CRT0066101 Chemical Structure

CRT0066101 Chemical Structure

CAS No. : 956123-34-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively[1]. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 has anticancer effects[2].

IC50 & Target[1][2]

PKD1

1 nM (IC50)

PKD2

2.5 nM (IC50)

PKD3

2 nM (IC50)

PIM2

135.7 nM (IC50)

体外研究
(In Vitro)

CRT0066101 (5 µM; 1 h) 可阻断 Panc-1 和 Panc-28 细胞中基础和 NT 诱导的 pS916-PKD1/2(激活的 PKD1/2)。CRT0066101 消除 NT 诱导的 Hsp27 (pS82-Hsp27) 磷酸化,减弱 PKD1 介导的 NF-κB 激活,并消除 NF-κB 依赖性增殖和促生存蛋白的表达[1] .
CRT0066101 显着抑制 Panc-1 细胞增殖,IC50 值为 1 µM。CRT0066101 可诱导 Panc-1 细胞凋亡 6-10 倍。CRT0066101 显着降低 Colo357、Panc-1、MiaPaCa-2 和 AsPC-1 细胞的增殖,但对 Capan-2 细胞有一定影响[1]

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

Western Blot Analysis[1]

Cell Line: Panc-1 and Panc-28 cells stimulation with neurotensin (NT)
Concentration: 5 µM
Incubation Time: 1 h
Result: Blocked both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2).
体内研究
(In Vivo)

CRT0066101(80 mg/kg/天;口服灌胃;每天一次;持续 21 天)在 Panc-1 原位模型中可有效阻止体内肿瘤生长[1]

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

Animal Model: CR-UK nu/nu mice injected with Panc-1 cells[1]
Dosage: 80 mg/kg/day
Administration: Oral gavage; once daily; for 21 days
Result: Potently blocked tumor growth in vivo.
分子量

338.41

Formula

C18H22N6O

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

CRT0066101 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)
× = ×
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:
CRT0066101
目录号:
HY-15698
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