CYC116

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

CYC116化学構造

CAS No. 693228-63-6

サイズ 価格(税別) 在庫状況
JPY 21900 国内在庫あり
JPY 63400 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(10)

カスタマーフィードバック1个实验数据

製品安全説明書

現在のバッチを見る: 純度: 99.52%
99.52

CYC116関連製品

Aurora Kinase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
U2OS cells Function assay 0.07-10 uM 2 h Inhibition of Aurora kinase in nocodazole-synchronized human U2OS cells assessed as reduction of histone H3 serine-10 phosphorylation at 0.07 to 10 uM after 2 hrs immunofluorescence microscopy 20462263
A549 cells Function assay 0.5-2 μM 7 h Cell cycle arrest in asynchronous human A549 cells assessed as accumulation of cyclin B1-negative tetraploid cells at G1 phase at 0.5 to 2 uM after 7 hrs by FACS analysis 20462263
SW620 cells Function assay 1 μM 48 h Effect on mitotic index in human SW620 cells assessed as appearance of polyploid cells at 1 uM after 48 hrs by propidium iodide staining-based FACS analysis 20462263
HeLa cells Function assay 1.25 μM 7 h Inhibition of Aurora kinase in human HeLa cells assessed as complete inhibition of histone H3 phosphorylation at 1.25 uM after 7 hrs by Western blot analysis 20462263
A2780 cells Cytotoxicity assay 96 h Cytotoxicity against human A2780 cells after 96 hrs by MTT assay 20462263
MIAPaCa2 cells Cytotoxicity assay 96 h Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay 20462263
HT-29 cells Cytotoxicity assay 96 h Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay 20462263
MCF7 cells Cytotoxicity assay 96 h Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay 20462263
HeLa cells Cytotoxicity assay 96 h Cytotoxicity against human HeLa cells after 96 hrs by MTT assay 20462263
COLO205 cells Cytotoxicity assay 96 h Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay 20462263
HCT116 cells Cytotoxicity assay 96 h Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay 20462263
K562 cells Cytotoxicity assay 96 h Cytotoxicity against human K562 cells after 96 hrs by MTT assay 20462263
CCRF-CEM cells Cytotoxicity assay 96 h Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay 20462263
MV4-11 cells Cytotoxicity assay 96 h Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay 20462263
HL60 cells Cytotoxicity assay 96 h Cytotoxicity against human HL60 cells after 96 hrs by MTT assay 20462263
NCI-H460 cells Cytotoxicity assay 96 h Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay 20462263
MESSA cells Cytotoxicity assay 96 h Cytotoxicity against human MESSA cells after 96 hrs by MTT assay 20462263
A549 cells Function assay 7 h Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy 20462263
BxPC3 cells Cytotoxicity assay 96 h Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay 20462263
HUPT4 cells Cytotoxicity assay 96 h Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay 20462263
Saos2 cells Cytotoxicity assay 96 h Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay 20462263
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 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
特性 An orally bioavailable, small molecule inhibitor of Aurora kinase/VEGFR2.
Targets
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
もっとクリックする
8 nM(Ki) 9 nM(Ki) 44 nM(Ki) 44 nM(Ki) 0.39 μM(Ki)
In Vitro
In vitro The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. [1] CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. [1] In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis. [1]
Kinase Assay Kinase Assays
Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO4, 10 μg of kemptide (peptide substrate)). Recombinant Aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl2, 100 μM ATP, with 18.5 kBq γ-32P-ATP per well) and incubated at 30°C for 30 minutes before termination with 25 μL of 75 mM H3PO4. Aurora B kinase assays are performed like Aurora A except that prior to use, Aurora B is activated in a separate reaction at 30°C for 60 minutes with inner centromere protein.
細胞実験 細胞株 HeLa, MCF7, MV4-11 and A2780 cells
濃度 0-10 μM
反応時間 72 or 96 hours
実験の流れ

Standard MTT assays are performed. In short, cells are seeded into 96-well plates according to doubling time and incubated overnight at 37°C. Test compounds are made up in DMSO, a 3-fold dilution series is prepared in 100 μL of cell medium, added to cells (in triplicates) and incubated for 72 or 96 hours at 37°C. MTT is made up as a stock of 5 mg/mL in cell medium, and the solution is filter-sterilized. Medium is removed from the cells followed by a wash with PBS. MTT solution is then added at 20 μL/well and incubated in the dark at 37°C for 4 hours. MTT solution is removed and cells are again washed with 200 μL of PBS. MTT dye is solubilized with 200 μL/well of DMSO by agitation. Absorbance is read at 540 nm and data analyzed using curve-fitting software to determine IC50 values.

In Vivo
In Vivo Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. [1]
動物実験 動物モデル NCI-H460 cells are implanted intraperitoneally into the mice.
投与量 75 and 100 mg/kg
投与経路 Administered via p.o.

化学情報

分子量 368.46 化学式

C18H20N6OS

CAS No. 693228-63-6 SDF Download CYC116 SDFをダウンロードする
Smiles CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4
保管

In vitro
Batch:

DMSO : 24 mg/mL ( (65.13 mM); Warmed with 50℃ water bath; 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。)

Water : Insoluble

Ethanol : 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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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)

mg/kg g μL

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。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: CYC116を買う | CYC116 ic50 | CYC116供給者 | CYC116を購入する | CYC116費用 | CYC116生産者 | オーダーCYC116 | CYC116化学構造 | CYC116分子量 | CYC116代理店