ホームページ Cell Cycle Aurora Kinase inhibitor - Bcr-Abl inhibitor - c-RET inhibitor - FGFR inhibitor - Autophagy activator - Apoptosis related activator - Trk receptor inhibitor Danusertib (PHA-739358) For research use only.

Danusertib (PHA-739358)

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.

Danusertib (PHA-739358)化学構造

CAS No. 827318-97-8

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Danusertib (PHA-739358)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
A2780 cells Proliferation assay Antiproliferative activity against A2780 cells, IC50=28 nM 17125279
HCT116 cells Proliferation assay Antiproliferative activity against HCT116 cells, IC50=31 nM 17125279
human HCT116 cells Proliferation assay Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs, IC50=31 nM 19320489
HCT116 cells Function assay Cell cycle arrest in HCT116 cells by accumulation at G2/M phase, EC50=80 nM 17125279
MCF7 cells Proliferation assay Antiproliferative activity against MCF7 cells, IC50=80 nM 17125279
HeLa cells Proliferation assay Antiproliferative activity against HeLa cells, IC50=0.14 μM 17125279
human MOLT4 cells Cytotoxic assay Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay, EC50=0.15 μM 22889561
human HepG2 cells Cytotoxic assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=4 μM 24910766
human A2780 cells Proliferation assay Antiproliferative activity against human A2780 cells assessed as accumulation of 4N DNA, IC50=28 μM 19320489
HCT116 cells Function assay Inhibition of histone h3 phosphorylation in HCT116 cells by Western blot analysis 17125279
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生物活性

製品説明 Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Targets
Aurora A [1]
(Cell-free assay)		 Abl [1]
(Cell-free assay)		 RET [1]
(Cell-free assay)		 TrkA [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 もっとクリックする
13 nM 25 nM 31 nM 31 nM 47 nM
In Vitro
In vitro Danusertib inhibits the activities of other kinases such as FGFR1, Abl, Ret and Trka, with IC50 of 47 nM, 25 nM, 31 nM and 31 nM, respectively. In a cell assay, after treatment of wild-type and p53-deficient MEFs with Danusertib, the wild-type cells undergo an arrest in mitosis (4N) that is maintained for up to 48 h. The p53-deficient cells on the other hand do not arrest at the 4N DNA stage, but continues with additional rounds of DNA synthesis to become >8N. Treatment with Danusertib results in an increase in p53 protein levels and an associated increase in p21 protein, which is known to be transcriptionally regulated by p53. [1] Increasing concentrations of Danusertib produces a dose-dependent reduction of cell growth after 48 hours in BCR-ABL-positive (K562, BV173) and BCR-ABL-negative (HL60) cells. [3]
Kinase Assay Biochemical kinase Assays
The Km values for ATP and the specific substrate are initially determined, and each assay is then run at optimized ATP (2Km) and substrate (5Km) concentrations. This setting enabled direct comparison of IC50 values of Danusertib across the applied kinase selectivity screening panel for the evaluation of the selectivity profile.
細胞実験 細胞株 CD34+ cells
濃度 5 μM
反応時間 5 days
実験の流れ For short-term expansion assays, 1 × 103 CD34+ cells are plated in triplicates in 96-well plates containing 100 μL of serum-free medium per well supplemented with human stem-cell factor (100 ng/mL), human Flt-3 Ligand (100 ng/mL), human thrombopoietin (50 ng/mL), human interleukin-3 and -6 (IL-3 and IL-6, respectively, both 20 ng/mL), and granulocyte colony-stimulating factor (20 ng/mL) along with Danusertib at the indicated concentrations. After 5 days, an additional 100 μL of cytokine and Danusertib containing medium are added. Cell numbers within each individual well are estimated on days 3, 6, and 9 or on days 3, 6, and 12 for healthy donor samples.
In Vivo
In Vivo Administration of 25 mg/kg Danusertib (b.d. i.v.) to HL-60 xenograft rats results in 75% inhibition of tumor growth with complete regression in one animal. Danusertib results in biomarker modulation accompanied by inhibition of tumor growth. This is compatible with an expected mechanism of action of aurora kinase inhibition. [1] Danusertib significantly inhibits proliferation of K562 cells and virtually suppressed tumor growth during the 10-day treatment period. [3]
動物実験 動物モデル Female SCID mice
投与量 15 mg/kg
投与経路 Intraperitoneally

化学情報

分子量 474.55 化学式

C26H30N6O3
CAS No. 827318-97-8 SDF Download Danusertib (PHA-739358) SDFをダウンロードする
Smiles CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=NNC4=C3CN(C4)C(=O)C(C5=CC=CC=C5)OC
保管

In vitro
Batch:

DMSO : 95 mg/mL ( (200.18 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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