EMD 534085
EMD 534085 Basic information
- Product Name:
- EMD 534085
- Synonyms:
-
- EMD 534085
- N-[2-(Dimethylamino)ethyl]-N'-[[(2R,4aS,5R,10bS)-3,4,4a,5,6,10b-hexahydro-5-phenyl-9-(trifluoromethyl)-2H-pyrano[3,2-c]quinolin-2-yl]methyl]urea
- CS-1076
- EMD534085; EMD-534085; EMD 534085.
- EMD 534085;EMD-534085
- 1-[[(2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl]methyl]-3-[2-(dimethylamino)ethyl]urea
- Urea, N-[2-(dimethylamino)ethyl]-N'-[[(2R,4aS,5R,10bS)-3,4,4a,5,6,10b-hexahydro-5-phenyl-9-(trifluoromethyl)-2H-pyrano[3,2-c]quinolin-2-yl]methyl]-
- 1-{[(2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-2H,3H,4H,4aH,5H,6H,10bH-pyrano[3,2-c]quinolin-2-yl]methyl}-3-[2-(dimethylamino)ethyl]urea
- CAS:
- 858668-07-2
- MF:
- C25H31F3N4O2
- MW:
- 476.53
- Mol File:
- 858668-07-2.mol
EMD 534085 Chemical Properties
- Boiling point:
- 609.5±55.0 °C(Predicted)
- Density
- 1.195
- storage temp.
- Store at -20°C
- solubility
- DMSO:26.0(Max Conc. mg/mL);54.56(Max Conc. mM)
- form
- A solid
- pka
- 13.78±0.46(Predicted)
- color
- White to off-white
EMD 534085 Usage And Synthesis
Uses
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
in vivo
In a low dose PK of EMD 534085 in mice the clearance is 1.8 L/h/kg on average, the volume of distribution is 7.4 L/kg and the half life around 2.5 h. The bioavailability in high dose experiments (>10 mg/kg) is always above 50% in mice. Intraperitonal administration of EMD 534085 enables significant systemic exposure in mice leading to a significant tumor growth reduction without toxic side effects[1].
IC 50
Kinesin-5: 8 nM (IC50)
References
[1] Schiemann K, et al. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. DOI:10.1016/j.bmcl.2010.01.110
[2] Tang Y, et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 2011 Nov 1;310(1):15-24. DOI:10.1016/j.canlet.2011.05.024
EMD 534085Supplier
- Tel
- sales@boylechem.com
- Tel
- +86 21 61551611
- Tel
- 021-58955995
- sales@medchemexpress.cn
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 021-61350663 13052117465
- sales@zehanbiopharma.com