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EMD534085
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EMD534085图片
CAS NO:858668-07-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
EMD534085是有效选择性的有丝分裂驱动蛋白-5 (kinesin-5)的抑制剂,IC50值为8 nM。
生物活性

EMD534085 is a potent and selective inhibitor of the mitotickinesin-5with anIC50of 8 nM.

IC50& Target[1]

Kinesin-5

8 nM (IC50)

体外研究
(In Vitro)

EMD 534085 does not inhibit any other tested kinesins (BimC, CEN-PE, Chromokinesin, KHC, KIF3C, KIFC3, MKLP-1, and MCAK) at 1 μM or 10 μM concentration, showing selectively over kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5[1]. EMD534085 induces rapid cell death in HL60 during mitotic arrest. Caspase-8, –9, –3, –7 are activated; Parp1 is cleaved; Mcl1 and XIAP are degraded in EMD534085-treated HL60 cells. EMD534085 treated HL60 cells also shows significantly accumulated phospho-Histone H3 level starting at 6 hrs post thymidine release[2].

体内研究
(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].

分子量

476.53

性状

Solid

Formula

C25H31F3N4O2

CAS 号

858668-07-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 26 mg/mL(54.56 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0985 mL10.4925 mL20.9850 mL
5 mM0.4197 mL2.0985 mL4.1970 mL
10 mM0.2099 mL1.0493 mL2.0985 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。