1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. CDK2-IN-47

CDK2-IN-47 是一种强效的 CDK2 抑制剂,其 IC50 为 0.21 μM。CDK2-IN-47 对 MCF-7、HCT-116 和 MGC-803 细胞系表现出优异的抗癌活性。CDK2-IN-47 可有效诱导 G1 细胞周期停滞、视网膜母细胞瘤蛋白 (Rb) 去磷酸化和显著的细胞凋亡 (apoptosis)。CDK2-IN-47 可用于乳腺癌、结直肠癌和胃癌的研究。

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CDK2-IN-47

CDK2-IN-47 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer[1].

IC50 & Target[1]

CDK2

0.21 μM (IC50)

CDK1

1.80 μM (IC50)

CDK7

8.70 μM (IC50)

CDK9

2.30 μM (IC50)

CDK4

> 10 μM (IC50)

CDK6

> 10 μM (IC50)

体外研究
(In Vitro)

CDK2-IN-47 (Compound 14c) (72 h) 对 MCF-7 (IC50 = 0.7 μM)、HCT-116 (IC50 = 1.1 μM) 和 MGC-803 (IC50 = 1.5 μM) 细胞系表现出优异的抗癌活性,并且对非癌性 HEK293 细胞具有显著的选择性 (SI = 22.4)[1]
CDK2-IN-47 (0.7 μM, 48 h) 在 MCF-7 细胞中诱导显著细胞凋亡[1]
CDK2-IN-47 (0.7 μM, 24 h) 在 MCF-7 中诱导 G0/G1 期细胞停滞细胞[1]
CDK2-IN-47 导致 MCF-7 细胞中 Ser807/811 位点 Rb 磷酸化显著降低[1]
CDK2-IN-47 在人肝微粒体中表现出较高的代谢稳定性 (t½ = 68.5 分钟,CLint = 8.5 mL/min/kg)[1]

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

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.7 μM
Incubation Time: 48 h
Result: Reached the apoptosis rate by 38.5%.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.7 μM
Incubation Time: 24 h
Result: Induced G0/G1 phase arrest reached 68.7%.
分子量

381.45

Formula

C16H23N5O4S

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:
CDK2-IN-47
目录号:
HY-178112
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