貨號	規格	價格	上海	北京	武漢	南京
S83346-5mg	98.6%	￥450.00 S83346-5mg ￥450.00 現貨	6 6	-	-	-
S83346-10mg	98.6%	￥590.00 S83346-10mg ￥590.00 現貨	7 7	-	-	-
S83346-25mg	98.6%	￥1010.00 S83346-25mg ￥1010.00 現貨	6 6	-	-	-
S83346-100mg	≥98%	￥2900.00 S83346-100mg ￥2900.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Empesertib (BAY1161909, Mps1-IN-5) 是一種三唑并吡啶的衍生物，是 serine/threonine monopolar spindle 1 (Mps1) kinase 的口服生物利用型選擇性抑制劑，IC50值 <1 nM。 Empesertib 具有潛在的抗腫瘤活性

產品描述：

靶點：

Mps1(Cell-free assay):1 nM;Kinesin

體外研究：

Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with an IC50 lower than or equal to 1 nM (more potent than 1 nM) in an Mps-1 kinase assay with a concentration of 1 μM/2 mM ATP, and an IC50 lower than 400 nM in a HeLa cell proliferation assay

體內研究：

Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with a maximum oral bioavailability (Fmax) in rat that is higher than 70%, determined by means of rat liver microsomes, and a maximum oral bioavailability (Fmax) in dog that is higher than 50%, determined by means of dog liver microsomes, and a maximum oral bioavailability (Fmax) in human that is higher than 60%, determined by means of human liver microsomes

細胞實驗：

Cell lines: Cultivated tumor cells Concentrations: 0.01 μM-30 μM Incubation Time: 4 days Method: Cultivated tumor cells are plated at a density of 5000 cells/well (MCF7, DU145, HeLa-MaTu-ADR), 3000 cells/well (NCI-H460, HeLa-MaTu, HeLa), or 1000 cells/well (B16F10) in a 96-well multititer plate in 200 μl of their 5 respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates was replaced by fresh culture medium (200 μl), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.01-30 μM; The cells are incubated for 4 days in the presence of test substances. Cell proliferation is determined by staining the cells with crystal violet: the cells are fixed by adding 20 μl/measuring point of an 11 % glutaric aldehyde solution for 15 minutes at room temperature. After three washing cycles of the fixed cells 15 with water, the plates are dried at

動物實驗：

Animal Models: rat, dog and humans Dosages: 1-2 mg/mL Administration: Oral gavage, IV

參考文獻：

1. Volker Schulze, et al. WO2014198647A2.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.787 ml	8.935 ml	17.87 ml
5 mM	0.357 ml	1.787 ml	3.574 ml
10 mM	0.179 ml	0.893 ml	1.787 ml
50 mM	0.036 ml	0.179 ml	0.357 ml

注意：

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

參考文獻

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Empesertib

(2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]-amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide; (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]