BAY 1217389

製品コードS8215 バッチS821502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H24F5N5O3
分子量 561.50 CAS No. 1554458-53-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (178.09 mM)
Ethanol (warmed with 50ºC water bath) 5 mg/mL (8.9 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile.
in vitro 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].
in vivo 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Tumor cell lines HeLa-MaTu and HeLa-MaTu-ADR cells
濃度 --
反応時間 96 h
実験の流れ 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.
動物実験 動物モデル Male Wistar rats and female CD1 or NMRI nu/nu mice
投薬量 1, 2, 4, or 8 mg/kg (p.o)
投与方法 i.v or p.o

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CDC7 inhibition induces replication stress-mediated aneuploid cells with an inflammatory phenotype sensitizing tumors to immune checkpoint blockade [ Nat Commun, 2023, 10.1038/s41467-023-43274-3] PubMed: 37980406
Loss of RanGAP1 drives chromosome instability and rapid tumorigenesis of osteosarcoma [ Dev Cell, 2023, 58(3):192-210.e11] PubMed: 36696903
Chromosomal instability can favor macrophage-mediated immune response and induce a broad, vaccination-like anti-tumor IgG response [ bioRxiv, 2023, 2023.04.02.535275] PubMed: 37066426
MPS1 inhibition primes immunogenicity of KRAS-LKB1 mutant lung cancer [ Cancer Cell, 2022, 40(10):1128-1144.e8] PubMed: 36150391
TTK Protein Kinase promotes temozolomide resistance through inducing autophagy in glioblastoma [ BMC Cancer, 2022, 22(1):786] PubMed: 35850753
TTK inhibition increases cisplatin sensitivity in high-grade serous ovarian carcinoma through the mTOR/autophagy pathway [ Cell Death Dis, 2021, 12(12):1135] PubMed: 34876569
Single-Chromosomal Gains Can Function as Metastasis Suppressors and Promoters in Colon Cancer. [ Dev Cell, 2020, 52(4):413-428] PubMed: 32097652
Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds [ Nature, 2019, 575(7781):203-209] PubMed: 31666698

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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