MLN0905

製品コードS2898 バッチS289802

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

C24H25F3N6S
分子量 486.56 CAS No. 1228960-69-7
Solubility (25°C)* 体外 DMSO 97 mg/mL (199.35 mM)
Water Insoluble
Ethanol Insoluble
* <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 MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.
in vitro MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. MLN0905 inhibits cell mitosis with EC50 of 9 nM. MLN0905 inhibits Cdc25C-T96 phosphorylation, a direct readout of PLK1 inhibition with EC50 of 29 nM. MLN0905 inhibits HT-29 viability with LD50 of 22 nM. MLN0905 possesses reasonable selectivity against a panel of 359 kinases. [1] MLN0905 inhibits a panel of lymphoma cells viability with IC50 of 3 – 24 nM. [2]
in vivo Nude mice bearing HT-29 xenografts administered with MLN0905 (6.25 mg/Kg - 50 mg/Kg, p.o.) shows dose-dependent pharmacodynamic responses (48 hours after treatment). OCI LY-19-Luc tumor bearing mice administered with MLN0905 (3.12 mg/Kg – 6.25 mg/Kg, p.o.) shows significant pharmacodynamic responses amd peaks at 8 hours after treatment. [1] MLN0905 shows antitumor efficacy in treatment with OCI LY-19-Luc xenografts bearing scid mice for 21 days. The T/C of 6.25 mg/Kg daily group is 0.15. [2]

プロトコル(参考用のみ)

キナーゼアッセイ PLK1 Flash Plate Assay
The human PLK1 enzymatic reaction totaling 30μL contained 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 0.02% BSA, 10% glycerol, 1 mM DTT, 100 mM NaCl, 3.3% DMSO, 8 μM ATP, 0.2μCi [γ- 33 P]-ATP, 4μM peptide substrate (Biotin-AHX-LDETGHLDSSGLQEVHLA-CONH2), and 10 nM recombinant human PLK1[2–369]T210D. The enzymatic reaction mixture, with or without PLK inhibitors, is incubated for 2.5 h at 30℃before termination with 20μL of 150 mM EDTA. Then 25μL of the stopped enzyme reaction mixture is transferred to a 384-well streptavidin coated Image FlashPlate and incubated at room temperature for 3 h. The Image Flash Plate wells are washed three times with 0.02% Tween-20 and then read on the Perkin-Elmer Viewlux.
細胞アッセイ 細胞株 HT-29
濃度
反応時間 72 h
実験の流れ Eight μL of serially diluted test compounds are added to75μL of HT29 (2.66 × 10 4 cells/well) cells in McCoy’s 5A media supplemented with 10% Fetal Calf Serum in Biocoat Poly-D lysine 384 well Black/Clear plates. Cells are incubated for 72 h at 37 ℃. Supernatant is aspirated from the wells, leaving 25μL in each well. ATP-lite 1 step reagent is added to each well, and luminescence for each plate is read on the LeadSeeker. Percent inhibition is calculated using the values from a DMSO control set to 100%.
動物実験 動物モデル Nude mice bearing HT-29 xenografts
投薬量 6.25 mg/Kg – 50 mg/Kg
投与方法 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：

The construction of drug-resistant cancer cell lines by CRISPR/Cas9 system for drug screening [L Zhang Science Bulletin, 2018, 10.1016/j.scib.2018.09.024]
Polo-like-kinase 1 is a proviral host-factor for hepatitis B virus replication. [Diab AM, et al. Hepatology, 2017, 10.1002/hep.29236] PubMed: 28445592

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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