ホームページ Cell Cycle Aurora Kinase inhibitor - VEGFR inhibitor CYC116 For research use only.

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

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代表番号: 045-509-1970|電子メール：[email protected]
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CYC116関連製品

シグナル伝達経路

Aurora Kinase Signaling Pathways

Aurora Kinaseシグナル伝達経路

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
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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 : 25 mg/mL ( (67.84 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。)

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 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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