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Tocris/RKI 1447 dihydrochloride/5061/50/50 mg

价格: ¥9180.00 市场价: 15300.00

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货号: 5061/50

品牌: Tocris

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Description: Potent and selective ROCK inhibitor; antitumor

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

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

Compound Libraries

RKI 1447 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	399.29
Formula	C₁₆H₁₄N₄O₂S.2HCl
Storage	Store at -20°C
Purity	≥99% (HPLC)
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	39.93	100
	water	3.99	10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 399.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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