R547
目录号 : KM3191 CAS No. : 741713-40-6 纯度 : 98%

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。

规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg 询价 In-stock
200mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

R547 is a potent, selective and oral orally bioavailable 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.

体外研究

R547 effectively inhibits CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1 (Ki = 1–3 nmol/L) and is inactive (Ki > 5,000 nmol/L) against a panel of >120 unrelated kinases in cell-free assays.
R547 effectively inhibits the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50s <0.60 μM.
R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest.
R547 has anti-proliferative activity in tumor cells independent of p53, retinoblastoma, or MDR status.
R547 blocks tumor cells in G1 plus G2 and induces apoptosis.
R547 induces apoptosis as measured by DNA fragmentation.
R547 inhibits phosphorylation of retinoblastoma protein in humantumor cells.

Cell Cytotoxicity Assay

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

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

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

R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing.
R547 inhibits phosphorylation of retinoblastoma protein in tumors.

Animal Model: 13-14 weeks old female immunodeficient nude mice (23-25 g), with HCT116/H460a/MDA-MB-435/DU145/LOX/A549 cells xenograft
Dosage: 40 mg/kg
Administration: Oral administration; daily; for 3-weeks
Result: Showed antitumor activity in all of the models in this study.
分子式
C18H21F2N5O4S
分子量
441.45
CAS号
741713-40-6
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (113.26 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2653 mL 11.3263 mL 22.6526 mL
5 mM 0.4531 mL 2.2653 mL 4.5305 mL
10 mM 0.2265 mL 1.1326 mL 2.2653 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.66 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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