RKI 1447 dihydrochloride

Cat. No. 5061 1 次引用提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Pricing	Availability		Qty

说明： Potent and selective ROCK inhibitor; antitumor

化学名： N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride

纯度： ≥99% (HPLC)

引用文献 (1)

文献 (3)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for RKI 1447 dihydrochloride

RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor (IC₅₀ values are 6.2 and 14.5 nM for ROCK2 and ROCK1 respectively); suppresses phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of Akt, MEK, and S6 kinase. Displays anti-invasive and antitumor activities in breast cancer cells. RKI 1447 dihydrochloride enhances the efficacy of BET inhibitors on the downregulation of N-Myc in vitro and in vivo.

化合物库 for RKI 1447 dihydrochloride

RKI 1447 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for RKI 1447 dihydrochloride

分子量	399.29
公式	C₁₆H₁₄N₄O₂S.2HCl
储存	Store at -20°C
纯度	≥99% (HPLC)
CAS Number	1782109-09-4
PubChem ID	90489001
InChI Key	GBXLRAPHQIRDNS-UHFFFAOYSA-N
Smiles	O=C(NCC3=CC=CC(O)=C3)NC1=NC(C2=CC=NC=C2)=CS1.Cl.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for RKI 1447 dihydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	3.99	10 温和加热
	DMSO	39.93	100

制备储备液 for RKI 1447 dihydrochloride

以下数据基于产品分子量 399.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.5 mL	12.52 mL	25.04 mL
5 mM	0.5 mL	2.5 mL	5.01 mL
10 mM	0.25 mL	1.25 mL	2.5 mL
50 mM	0.05 mL	0.25 mL	0.5 mL

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产品说明书 for RKI 1447 dihydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for RKI 1447 dihydrochloride

参考文献是支持产品生物活性的出版物。

Patel et al (2012) RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 72 5025 PMID: 22846914

Pireddu et al (2013) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2) Med.Chem.Comm. 3 699 PMID: 23275831

Pepich et al (2024) The ROCK-1/2 inhibitor RKI-1447 blocks N-MYC, promotes cell death, and emerges as a synergistic partner for BET inhibitors in neuroblastoma. Cancer Lett. PMID: 39307412

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关键词: RKI 1447 dihydrochloride, RKI 1447 dihydrochloride supplier, RKI1447, dihydrochloride, Potent, and, selective, ROCK, inhibitors, inhibits, anti-invasive, antitumor, breast, cancer, ROCK1, ROCK2, MLC-2, MYPT-1, in, vivo, Rho-kinases, 5061, Tocris Bioscience

1 篇 RKI 1447 dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 RKI 1447 dihydrochloride 的部分引用包括：

Pepich et al (2024) The ROCK-1/2 inhibitor RKI-1447 blocks N-MYC, promotes cell death, and emerges as a synergistic partner for BET inhibitors in neuroblastoma. Cancer Lett. PMID: 39307412

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