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

R547 是一種高效、選擇性的，口服有效的 ATP 競爭性的 CDK 抑制劑，對 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的 Ki 值分別為 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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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥823
In-stock
5 mg ￥1812
In-stock
10 mg ￥2900
In-stock
25 mg ￥4500
In-stock
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500 mg 現(xiàn)貨 詢價
1 g   詢價  
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Customer Review

Other Forms of R547:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

體外研究
(In Vitro)

R547 有效抑制 CDK1/細胞周期蛋白 B、CDK2/細胞周期蛋白 E 和 CDK4/細胞周期蛋白 D1 (Ki=1-3 nM)，并且對細胞中 >120 種不相關(guān)的激酶無活性 (Ki> 5,000 nM)[4]。
R547 有效抑制腫瘤細胞系的增殖，不受多藥耐藥狀態(tài)、組織學(xué)類型、視網(wǎng)膜母細胞瘤蛋白或 p53 狀態(tài)的影響，IC50 <0.60 μM[4]。
R547 在誘導(dǎo)細胞周期停滯的相同濃度下降低細胞視網(wǎng)膜母細胞瘤蛋白在特定 CDK 磷酸化位點的磷酸化[4]。
R547 在腫瘤細胞中具有抗增殖活性，與 p53、視網(wǎng)膜母細胞瘤或 MDR 狀態(tài)無關(guān)[4]。
R547 阻斷 G1 和 G2 和 G2 中的腫瘤細胞誘導(dǎo)細胞凋亡[4]。
R547 通過 DNA 片段化測量誘導(dǎo)細胞凋亡[4]。
R547 抑制人腫瘤細胞中視網(wǎng)膜母細胞瘤蛋白的磷酸化[4]。

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

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.
體內(nèi)研究
(In Vivo)

R547 具有顯著的體內(nèi)療效，每日口服和每周靜脈注射一次[4]。
R547 抑制腫瘤中視網(wǎng)膜母細胞瘤蛋白的磷酸化[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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
純度 & 產(chǎn)品資料

純度: 99.57%

參考文獻

  • 摩爾計算器

  • 稀釋計算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量   濃度   體積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (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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產(chǎn)品名稱：
R547
目錄號：
HY-10014
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