貨號	規(guī)格	價格	上海	北京	武漢	南京
S34152-5mg	98.7%	￥500.00 S34152-5mg ￥500.00 現(xiàn)貨	2 2	-	-	-
S34152-10mg	98.7%	￥730.00 S34152-10mg ￥730.00 現(xiàn)貨	3 3	-	-	-
S34152-25mg	98.7%	￥1240.00 S34152-25mg ￥1240.00 現(xiàn)貨	2 2	-	-	-
S34152-100mg	98.7%	￥3600.00 S34152-100mg ￥3600.00 現(xiàn)貨	1 1	-	-	-

產(chǎn)品介紹

MELK-8a hydrochloride是一種新穎的母體胚胎亮氨酸拉鏈激酶（MELK）抑制劑，其IC50值為2 nM。

產(chǎn)品描述：

MELK-8a hydrochloride是一種新穎的母體胚胎亮氨酸拉鏈激酶（MELK）抑制劑，其IC50值為2 nM。

靶點：

IC50: 2 nM (MELK);MELK

體外研究：

MELK-8a remains very potent (IC50=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2 μM, respectively.

體內(nèi)研究：

Subcutaneous administration of MELK-8a at 30 mg/kg in C57BL/6 mice results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (Tmax=0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, when administered orally at 10 mg/kg in C57BL/6 male mice, it shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance.

參考文獻：

1. Touré BB, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.132 ml	10.661 ml	21.321 ml
5 mM	0.426 ml	2.132 ml	4.264 ml
10 mM	0.213 ml	1.066 ml	2.132 ml
50 mM	0.043 ml	0.213 ml	0.426 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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MELK-8a hydrochloride