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
- Molecular Weight:
- 476.53
- MDL Number:
- MOL File:
- 858668-07-2.mol
| 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 |
| FDA UNII | AL67QX8036 |
EMD 534085 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-6279 | EMD534085 99.03% | 858668-07-2 | 1mg | $90 | 2021-12-16 | Buy |
| ChemScene | CS-6279 | EMD534085 99.03% | 858668-07-2 | 5mg | $270 | 2021-12-16 | Buy |
| ChemScene | CS-6279 | EMD534085 99.03% | 858668-07-2 | 10mg | $450 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | INB0000565 | EMD 534085 95.00% | 858668-07-2 | 5MG | $495.64 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb180978 | EMD534085 >98% | 858668-07-2 | 10mg | $838.1 | 2021-12-16 | Buy |
EMD 534085 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30230 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2922 | 55 | |
| Shanghai T&W Pharmaceutical Co., Ltd. | +86 21 61551611 | China | 9891 | 58 | |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4861 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4621 | 55 | |
| Shanghaizehan biopharma technology co., Ltd. | 021-61350663 13052117465 | sales@zehanbiopharma.com | China | 998 | 55 |