货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57884-1ml	10mM in DMSO	￥11320.00 V57884-1ml ￥11320.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57884-1ml

10mM in DMSO

￥11320.00

货期：3-5天

产品描述：

WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM.

体外研究：

WDR5-IN-5 (compound 41) (10 mg/kg; p.o.) shows high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h[1].

WDR5-IN-5 (3 mg/kg; i.v.) also shows low iv clearance (26 mL/min/kg). WDR5-IN-5 is well tolerated and shows no adverse effects in mice by both i.v. and p.o. dosing[1].

WDR5-IN-5 can be formulated as 0.6 and 1 mg/mL solutions in ethanol, tocopherol poly (ethylene glycol) succinate (TPGS), PEG400 and water (v/v/v/v, 5/5/30/60) for i.v. and p.o. dosing, respectively[1].

PK profile of WDR5-IN-5 in CD-1 Mice[1]

体内研究：

WDR5 plays an important role in the activity of MLL1 histone methyltransferase (HMT) complexes. WDR5-IN-5 (compound 41), as a WDR5 inhibitor, will exihibits inhibitory effect towards HMT.

WDR5-IN-5 displays average soluble concentrations (kinetic solubility) of 60 μM.

WDR5-IN-5 exhibits high selectivity between K562 cells and MV4:11, the selectivity index (GI50, K562/GI50, MV4:11) is 290.

WDR5-IN-5 (0-30 μM; 5 d) inhibits cell proliferation of MV4:11, MOLM-13, and K562 with GI50 values are 13, 27, 3700 nM, respectively.

保存条件：

-80°C 6个月;-20°C 1个月

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.871 ml	9.353 ml	18.706 ml
5 mM	0.374 ml	1.871 ml	3.741 ml
10 mM	0.187 ml	0.935 ml	1.871 ml
50 mM	0.037 ml	0.187 ml	0.374 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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