218716
Casein Kinase I Inhibitor II, PF-670462
4-(3-Cyclohexyl-5-(4-fluorophenyl)-3H-imidazol-4-yl)-pyrimidin-2-ylamine, 2HCl
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
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Fax: +49 6151 72 2000
31 May 2012
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A cell-permeable tri-substituted imidazole compound that acts as a potent and reversible inhibitor of casein kinase Iε/δ (IC50 = 7.7 and 14 nM, respectively) with modest to excellent selectivity over EGFR and p38 MAPK (IC50 = 150 and 190 nM, respectively) and over 43 related kinases (IC50 > 0.3 to 30 µM), and a panel containing 116-receptors, transporters and other enzymes. Shown to inhibit PER3 nuclear translocation in GFP-PER3 and CKIε-cotransfected COS7 cells (EC50 = 290 nM), and induce phase delays in circadian rhythms of monkeys & rats model (10 - 100 mg, s.c.); further, attenuate the locomotor stimulant response to methamphetamine.
| Product information | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Molar mass | 410.32 | ||
| Protect from Light | Yes | ||
| Hygrocopic | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO or H2O | ||
| Chemical formula | C19H20FN5 • 2HCl | ||
| CAS number | 950912-80-8 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 22-24/25-36/37/39 Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing, gloves and eye/face protection. |
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