2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Stem Cell/Wnt Apoptosis
  3. CDK GSK-3 Apoptosis
  4. R547

R547 是一种高效、选择性的，口服有效的 ATP 竞争性的 CDK 抑制剂，对 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的 Ki 值分别为 2 nM、3 nM、1 nM。

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R547 Chemical Structure

R547 Chemical Structure

CAS No. : 741713-40-6

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Other Forms of R547:

R547 相关抗体

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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GSK-3 GSK-3α GSK-3β

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively[1][2][3][4][5].

IC50 & Target[1]

Cdk1/cyclin B

2 nM (Ki)

CDK2/cyclinE

3 nM (Ki)

CDK4/cyclin D

1 nM (Ki)

cdk2/cyclin A

0.1 nM (IC50)

CDK2/cyclinE

0.4 nM (IC50)

Cdk1/cyclin B

0.2 nM (IC50)

CDK3/Cyclin E

0.8 nM (IC50)

CDK5/p35

0.1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

CDK7/cyclin H

171 nM (IC50)

GSK-3α

46 nM (IC50)

GSK-3β

260 nM (IC50)

体外研究
(In Vitro)

R547 有效抑制 CDK1/细胞周期蛋白 B、CDK2/细胞周期蛋白 E 和 CDK4/细胞周期蛋白 D1 (Ki=1-3 nM)，并且对细胞中 >120 种不相关的激酶无活性 (Ki> 5,000 nM)[4]。
R547 有效抑制肿瘤细胞系的增殖，不受多药耐药状态、组织学类型、视网膜母细胞瘤蛋白或 p53 状态的影响，IC50 <0.60 μM[4]。
R547 在诱导细胞周期停滞的相同浓度下降低细胞视网膜母细胞瘤蛋白在特定 CDK 磷酸化位点的磷酸化[4]。
R547 在肿瘤细胞中具有抗增殖活性，与 p53、视网膜母细胞瘤或 MDR 状态无关[4]。
R547 阻断 G1 和 G2 和 G2 中的肿瘤细胞诱导细胞凋亡[4]。
R547 通过 DNA 片段化测量诱导细胞凋亡[4]。
R547 抑制人肿瘤细胞中视网膜母细胞瘤蛋白的磷酸化[4]。

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

R547 相关抗体:

Cell Cytotoxicity Assay[4]

Cell Line: Human tumor cell lines (MDA-MB-468, MDA-MB-435, MCF-7, HCT116, SW480, RKO, HT-29, HCT15, H460a, C33A, DU145, OSA-CL, LOX, JEKO-1, REC-1)
Concentration: MTT assay
Incubation Time: 5 days
Result: Has potent in vitro antiproliferative activity.

Cell Cycle Analysis[4]

Cell Line: R547, HCT116
Concentration: 0.1 μM, 0.2 μM, 0.6 μM
Incubation Time: 20 hours
Result: Decrease in BrdUrd incorporation and in percentage S phase in a dose-dependent, indicative of a cell cycle block in G1-S plus G2-M.

Western Blot Analysis[4]

Cell Line: HCT116 cells
Concentration: 0.1 μM, 0.2 μM, 0.6 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Showed a band corresponding to a p48/retinoblastoma fragment that becomes more intense at 48 and 72 hours.
体内研究
(In Vivo)

R547 具有显著的体内疗效，每日口服和每周静脉注射一次[4]。
R547 抑制肿瘤中视网膜母细胞瘤蛋白的磷酸化[4]。

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

Animal Model: 13-14 weeks old female immunodeficient nude mice (23-25 g), with HCT116/H460a/MDA-MB-435/DU145/LOX/A549 cells xenograft[4]
Dosage: 40 mg/kg
Administration: Oral administration; daily; for 3-weeks
Result: Showed antitumor activity in all of the models in this study.
分子量

441.45

Formula

C18H21F2N5O4S
CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
纯度 & 产品资料

纯度: 99.57%

COA (290 KB) LCMS (136 KB)

产品使用指南 (1538 KB)
参考文献

R547 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 *
= × ×

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.

Keywords:

R547741713-40-6R 547R-547CDKGSK-3ApoptosisCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3cyclin-dependentkinasemultiplehumantumorInhibitorinhibitorinhibit

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目录号：
HY-10014
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