Onvansertib (NMS-1286937, NMS-P937)

別名：PCM-075, NMS1286937

製品コード：S7255 純度：99.83%

Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.

CAS No. 1034616-18-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 44800	国内在庫あり
10mg	JPY 41800	国内在庫あり
50mg	JPY 118500	国内在庫あり
1g	JPY 745500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（13）

製品安全説明書

現在のバッチを見る：純度： 99.83%

99.83

Onvansertib (NMS-1286937, NMS-P937)関連製品

関連ターゲット	PLK1 PLK2 PLK3 PLK4	もっと見る
関連製品	BI 2536 Volasertib (BI6727) Rigosertib (ON-01910) GSK461364 SBE 13 HCl Ro3280 CFI-400945 HMN-214 MLN0905 Poloxin	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

PLKシグナル伝達経路

PLK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
CAL51	Cell cycle assay	0.1 to 1 uM	24 hrs	Cell cycle arrest in human CAL51 cells at 0.1 to 1 uM after 24 hrs by flow cytometry	21470862
A2780	Antiproliferative assay			Antiproliferative activity against human A2780 cells, IC50 = 0.042 μM.	21470862
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

PLK1 ^[1]

2 nM

In Vitro
In vitro	Onvansertib (NMS-1286937, NMS-P937) shows a broad-spectrum antiproliferative activity against different solid tumor, leukemias and lymphomas cell lines. It potently causes a mitotic cell-cycle arrest followed by apoptosis in A2780 cells. ^[2]
Kinase Assay	Kinase profile
Kinase Assay	Onvansertib (NMS-1286937, NMS-P937) inhibitory activity and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with ³³P-γ-ATP, at optimized buffer and cofactors conditions. At the end of the phosphorylation reaction, more than 98% unlabeled ATP and radioactive ATP is captured by adding an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity. Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting. Inhibitory potency evaluation for all the tested kinases was performed at 25 °C using a 60 min end-point assay where the concentrations of ATP and substrates are kept equal to 2 x αKm and saturated (>5 x αKm), respectively.
細胞実験	細胞株	137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomas
	濃度	~10 μM
	反応時間	72 hours
	実験の流れ	Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells were treated in duplicate with serial dilutions of Onvansertib (NMS-1286937, NMS-P937), and 72 hours later, the viable cell number was assessed by the CellTiter-Glo Assay (Promega). IC50 values were calculated with a sigmoidal fitting algorithm (Assay Explorer MDL). Experiments were carried out independently at least twice.

In Vivo
In Vivo	Onvansertib (NMS-1286937, NMS-P937) shows significant tumor growth inhibition in mice xenografted with human HCT116 colon adenocarcinoma cells at 90 mg/kg/d i.v. or p.o. ^[1] In mice bearing HT29, Colo205 colorectal, or A2780 ovarian xenograft tumors, it inhibits xenograft tumor growth. In addition, this compound, in combination with approved cytotoxic drugs, causes enhanced tumor regression and prolongs survival of animals. ^[2]

In Vivo

Onvansertib (NMS-1286937, NMS-P937) shows significant tumor growth inhibition in mice xenografted with human HCT116 colon adenocarcinoma cells at 90 mg/kg/d i.v. or p.o. ^[1]

In mice bearing HT29, Colo205 colorectal, or A2780 ovarian xenograft tumors, it inhibits xenograft tumor growth. In addition, this compound, in combination with approved cytotoxic drugs, causes enhanced tumor regression and prolongs survival of animals. ^[2]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05593328	Active not recruiting	Colorectal Cancer\|Metastatic Colorectal Cancer	Cardiff Oncology	March 17 2023	Phase 2
NCT03829410	Completed	Metastatic Colorectal Cancer\|KRAS Gene Mutation	Cardiff Oncology	May 6 2019	Phase 1\|Phase 2
NCT03303339	Completed	Acute Myeloid Leukemia	Cardiff Oncology	November 17 2017	Phase 1\|Phase 2

参考
https://pubmed.ncbi.nlm.nih.gov/21470862/ https://pubmed.ncbi.nlm.nih.gov/22319201/

参考

https://pubmed.ncbi.nlm.nih.gov/21470862/
https://pubmed.ncbi.nlm.nih.gov/22319201/

化学情報

分子量	532.52	化学式	C₂₄H₂₇F₃N₈O₃
CAS No.	1034616-18-6	SDF	Download Onvansertib (NMS-1286937, NMS-P937) SDFをダウンロードする
Smiles	CN1CCN(CC1)C2=CC(=C(C=C2)OC(F)(F)F)NC3=NC=C4CCC5=C(C4=N3)N(N=C5C(=O)N)CCO
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 42 mg/mL ( (78.87 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 10 mg/mL

Water : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.				投与溶液組成計算機
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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