R547|cas:741713-40-6|西域试剂

R547,99.57%

产品编号：Bellancom-10014| CAS NO：741713-40-6| 分子式：C₁₈H₂₁F₂N₅O₄S| 分子量：441.45

R547是ATP竞争性CDK1，2，4抑制剂，Ki分别为2 nM，3 nM和1 nM。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-10014		￥2900.00	杭州北京（现货）
Bellancom-10014		￥8500.00	杭州北京（现货）

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R547

产品介绍

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 K_i 值分别为 2 nM、3 nM、1 nM。

生物活性

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

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^[4].
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^[4].
R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest^[4].
R547 has anti-proliferative activity in tumor cells independent of p53, retinoblastoma, or MDR status^[4].
R547 blocks tumor cells in G1 plus G2 and induces apoptosis^[4].
R547 induces apoptosis as measured by DNA fragmentation^[4].
R547 inhibits phosphorylation of retinoblastoma protein in humantumor cells^[4].

西域 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.

体内研究
(In Vivo)

R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing^[4].
R547 inhibits phosphorylation of retinoblastoma protein in tumors^[4].

西域 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.

体内研究

R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing^[4].
R547 inhibits phosphorylation of retinoblastoma protein in tumors^[4].

西域 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.

体内研究

R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing^[4].
R547 inhibits phosphorylation of retinoblastoma protein in tumors^[4].

西域 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.

性状

Solid

溶解性数据

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

参考文献

. Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N.Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4 [Content Brief]

. Bayés M, Rabasseda X, Prous JR.Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jul-Aug;29(6):427-37. [Content Brief]

. Martin F, Thomson TM, Sewer A, Drubin DA, Mathis C, Weisensee D, Pratt D, Hoeng J, Peitsch MC.Assessment of network perturbation amplitudes by applying high-throughput data to causal biological networks.BMC Syst Biol. 2012 May 31;6:54. [Content Brief]

[4]. DePinto, Wanda et al In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials Molecular Cancer Therapeutics (2006), 5(11), 2644-2658 [Content Brief]

[5]. Jones, Clifford D.; Andrews, David M. Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors Bioorganic & Medicinal Chemistry Letters (2008), 18(24), 6486-6489 [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

危险品运输编码	NONH for all modes of transport

1. 物质的识别

产品名：	R547
CAS号：	741713-40-6
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	R547
分子式：	C18H21F2N5O4S
分子量：	441.45

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。