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BAY1217389
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。
BAY1217389图片
CAS NO:1554458-53-5
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
BAY1217389 是一种有效的选择性单极纺锤体 1 (MPS1) 激酶抑制剂 ,IC50值小于10 nM。
In biochemical assays, the IC50 value of BAY 1217389 is 0.63±0.27 nmol/L. It shows high selectivity against other kinases and found to bind to PDGFRβ (<10 nmol/L), Kit (between 10 and 100 nmol/L), CLK1, CLK2, CLK4, JNK1, JNK2, JNK3, LATS1, MAK, MAPKAP2, MERTK, p38β, PDGFRα, PIP5K1C, PRKD1, and RPS6KA5 (between 100 and 1,000 nmol/L). In cellular mechanistic assays, BAY1217389 abrogats nocodazole-induced SAC activity and induced premature exit from mitosis ("mitotic breakthrough"), resulting in multinuclearity and tumor cell death. It is found to inhibit cell proliferation with a median IC50 of 6.7 nmol/L (range 3 to >300 nmol/L)[1].

产品描述

BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).

体外活性

In biochemical assays, the IC50 value of BAY 1217389 is 0.63±0.27 nmol/L. It shows high selectivity against other kinases and found to bind to PDGFRβ (<10 nmoll), kit (between 10 and 100 clk1,clk2, clk4, jnk1, jnk2, jnk3, lats1, mak, mapkap2, mertk, p38β, pdgfrα, pip5k1c, prkd1, rps6ka5 1,000 l). in cellular mechanistic assays, bay1217389 abrogatsnocodazole-induced sac activity induced premature exit from mitosis ("mitotic breakthrough"), resulting multinuclearity tumor cell death. it is found to inhibit proliferation with a median ic50 of 6.7 l (range 3>300 nmol/L)[1].

体内活性

In vivo, BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. Its blood clearance is found to be low in the tested species. Vss is high and terminal half-lives were long. BAY 1217389 is administered orally to female NMRI mouse (1 mg/kg) and male Wistar rat (0.5 mg/kg). Peak plasma concentrations are observed between 1.5 and 7 hours. Oral bioavailability is high in rat and moderate in mouse[1].

激酶实验

Inhibition of recombinant human Mps1 by BAY 1161909 or BAY 1217389 is assessed in TRFRET-based in vitro kinase assays via phosphorylation of a biotinylated peptide (Biotin-Ahx-PWDPDDADITEILG-NH2). Under standard assay conditions kinase and test compound are preincubated for 15 min before enzyme reaction is started by addition of substrate and ATP upon 10 μM[1].

细胞实验

Cells are seeded into 96-well plates at densities ranging from 1,000 to 5,000 cells per well in the appropriate medium supplemented with 10% FCS. After 24 hours, cells are treated in quadruplicates with serial dilutions of compounds. After further 96 hours, adherent cells are fixed with glutaraldehyde and stained with crystal violet. IC50 values are calculated by means of a 4-parameter fit using the company's own software.(Only for Reference)

Cas No.

1554458-53-5

分子式

C27H24F5N5O3

分子量

561.513

储存和溶解度

DMSO:93 mg/mL (165.6 mM)
H2O:<1 mgml
Ethanol:3 mg/mL (5.34 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years