BI 2536

製品コードS1109 バッチS110906

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₈H₃₉N₇O₃

分子量

521.66

CAS No.

755038-02-9

Solubility (25°C)*

体外

DMSO

100 mg/mL (191.69 mM)

Ethanol

50 mg/mL (95.84 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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.
Clear solution	5%DMSO 1 5%Tween80 2 90%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.300mg/ml (6.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 66 mg/ml clarified DMSO stock solution to 50 μL of Tween80, mix evenly to clarify; then continue to add 900 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.000mg/ml (3.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
in vitro	BI 2536 blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 nM, respectively. In HeLa cells, this compound treatment ranging from 10-100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, as well as a range of other mitotic processes that are known to depend on Plk1. This chemical treatment leads to the HeLa cells arrested in G2/M, subsequently a sub-G1 DNA peak indicative of DNA breakdown and apoptosis, and accumulated cleaved PARP p85 fragments in a concentration-dependent manner. It inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM, while blocking the proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells with EC50 of 12-31 nM. ^[1] Plk1 inhibition by this compound reduces the growth and viability of anaplastic thyroid carcinoma (ATC) cells such as CAL62, OCUT-1, SW1736, 8505C, and ACT-1 with EC50 values of 1.4-5.6 nM. ^[2]
in vivo	BI 2536 given i.v. once or twice per week is highly efficacious in diverse xenograft models with acceptable tolerability by inhibiting cell proliferation through a mitotic arrest, and subsequently induction of tumor-cell death. Administration of this compound at 50 mg/kg once or twice per week significantly inhibits growth of HCT 116 xenografts with T/C of 15% and 0.3%, respectively. This chemical treatment twice-weekly also leads to excellent tumor-growth in BxPC-3 and A549 models with T/C of 5% and 14%, respectively. ^[1]
特徴	The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition.

プロトコル(参考用のみ)

キナーゼアッセイ	Plk1 in vitro kinase assay
キナーゼアッセイ	Recombinant human Plk1 (residues 1-603) is expressed as N-terminal, GST-tagged fusion protein with a baculoviral expression system and purified by affinity chromatography with Glutathione-agarose. Enzyme activity assays for Plk1 are performed in the presence of serially diluted BI 2536 with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions are performed in a final volume of 60 μL for 45 minutes at 30 °C (15 mM MgCl₂, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-³³P-ATP). Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transfer of the precipitates to Multi-Screen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curve is used for calculating IC50 value.
細胞アッセイ	細胞株	HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells, etc.
	濃度	Dissolved in DMSO, final concentrations ~1 μM
	反応時間	24 and 72 hours
	実験の流れ	Cells are exposed to various concentrations of BI 2536 for 24, and 72 hours. Cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. For determining the DNA content of the cultures, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide (PI) in PBS for 20 minutes at RT. Cell-cycle profiles are determined by flow cytometric analysis.
動物実験	動物モデル	Female BomTac:NMRI-Foxn1^nu mice injected subcutaneously with HCT 116, NCI-H460, or A549 cells
	投薬量	~50 mg/kg
	投与方法	Injection i.v. once or twice per week

参考

https://pubmed.ncbi.nlm.nih.gov/17291758/
https://pubmed.ncbi.nlm.nih.gov/19223553/
https://pubmed.ncbi.nlm.nih.gov/26191363/

カスタマーフィードバック

: Data from [J Biomol Screen, 2013, 18(1), 54-66]

: Data from [J Biomol Screen, 2013, 18(1), 54-66]

: Data from [J Biol Chem, 2012, 287(21), 17088-99]

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：

DNAJ-PKAc fusion heightens PLK1 inhibitor sensitivity in fibrolamellar carcinoma [ Gut, 2025, gutjnl-2024-334274]	PubMed: 40274389
Spatio-temporal control of mitosis using light via a Plk1 inhibitor caged for activity and cellular permeability [ Nat Commun, 2025, 16(1):1599]	PubMed: 39971898
ZSCAN4 functions as a safeguard to maintain centromere integrity during oocyte meiosis [ Genome Biol, 2025, 26(1):204]	PubMed: 40665375
CDK1-mediated phosphorylation of LDHA fuels mitosis through LDHB-dependent lactate oxidation [ EMBO Rep, 2025, 10.1038/s44319-025-00573-8]	PubMed: 40940446
Overexpression of oncogenic polo-like kinase 1 disrupts the invasiveness, cell cycle, and apoptosis in synovial sarcoma [ J Transl Med, 2025, 23(1):691]	PubMed: 40542346
Preparation for mitosis requires gradual CDK1 activation [ iScience, 2025, 28(5):112292]	PubMed: 40256327
Revisiting phosphoregulation of Cdc25C during M-phase induction [ iScience, 2025, 28(1):111603]	PubMed: 39834856
Azenosertib is a potent and selective WEE1 kinase inhibitor with broad antitumor activity across a range of solid tumors [ Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-24-1194]	PubMed: 40231599
Staphylococcus aureus utilizes vimentin to internalize human keratinocytes [ Front Cell Infect Microbiol, 2025, 15:1543186]	PubMed: 40061451
Aurora B maintains spherical shape of mitotic cells via simultaneously stabilizing myosin II and vimentin [ J Mol Cell Biol, 2025, mjaf023]	PubMed: 40795355

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。