EMD 534085
- Product Name
- EMD 534085
- CAS No.
- 858668-07-2
- Chemical Name
- EMD 534085
- Synonyms
- CS-1076;EMD 534085;EMD 534085;EMD-534085;EMD534085; EMD-534085; EMD 534085.;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;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;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;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]-
- CBNumber
- CB42602596
- Molecular Formula
- C25H31F3N4O2
- Formula Weight
- 476.53
- MOL File
- 858668-07-2.mol
EMD 534085 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-6279
- Product name
- EMD534085
- Purity
- 99.03%
- Packaging
- 1mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-6279
- Product name
- EMD534085
- Purity
- 99.03%
- Packaging
- 5mg
- Price
- $270
- Updated
- 2021/12/16
- Product number
- CS-6279
- Product name
- EMD534085
- Purity
- 99.03%
- Packaging
- 10mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- INB0000565
- Product name
- EMD 534085
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $495.64
- Updated
- 2021/12/16
- Product number
- orb180978
- Product name
- EMD534085
- Purity
- >98%
- Packaging
- 10mg
- Price
- $838.1
- Updated
- 2021/12/16
EMD 534085 Chemical Properties,Usage,Production
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 534085 Preparation Products And Raw materials
Raw materials
Preparation Products
EMD 534085 Suppliers
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- +86 21 61551611
- Fax
- +86 21 50676805
- Country
- China
- ProdList
- 9891
- Advantage
- 58
- Tel
- 021-58955995
- Fax
- 609-228-5909
- sales@medchemexpress.cn
- Country
- United States
- ProdList
- 4861
- Advantage
- 58
- Tel
- 021-52996696,15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4827
- Advantage
- 55
- Tel
- 021-61350663 13052117465
- Fax
- 021-61350662
- sales@zehanbiopharma.com
- Country
- China
- ProdList
- 977
- Advantage
- 55
- Tel
- 0570-3081766 18357083060
- Fax
- 0570-3072337
- sales@qzamkbio.com
- Country
- China
- ProdList
- 1156
- Advantage
- 55
- Tel
- 0371-53778726 18003825608
- Fax
- 2885354392
- liuxiaoyan@alfachem.cn
- Country
- China
- ProdList
- 1988
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 86249
- Advantage
- 60
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 7999
- Advantage
- 62
- Tel
- +86 18721201413
- Fax
- +86 (21) 5775-8967
- sales@biopharmaleader.com
- Country
- China
- ProdList
- 1720
- Advantage
- 58