BI 2536 (Synonyms: BI-2536;BI2536) |
| Catalog No.GC12450 |
BI 2536, dual Polo-like kinase (PLK)/bromodomain inhibitors, effectively reactivate latent HIV-1. Half maximal inhibitory concentration (IC50) values of BI 2536 against PLK1, PLK2, and PLK3 in cell-free kinase assays are 0.83nM, 3.5nM and 9.0nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 755038-02-9
Sample solution is provided at 25 µL, 10mM.
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BI 2536, dual Polo-like kinase (PLK)/bromodomain inhibitors, effectively reactivate latent HIV-1. Half maximal inhibitory concentration (IC50) values of BI 2536 against PLK1, PLK2, and PLK3 in cell-free kinase assays are 0.83nM, 3.5nM and 9.0nM, respectively[1].
In vitro, BI 2536 (0.1, 0.5, 1 and 2μM; 72h) inhibited the proliferation of ovarian cancer cells and induced cell cycle arrest at the G2/M phases[2]. BI 2536 (28.23 and 17.30nM; 24 and 48h) promotes neuroblastoma cell death via minichromosome maintenance complex components 2 and 10[3]. Alisertib cooperates with BI 2536 (14h and 24h) to induce cell cycle arrest and DNA double-strand breaks in small cell lung cancer[4]. BI 2536 (5nM and 10nM; 24h) induces apoptosis and attenuates the autophagic process in neuroblastoma cells[5].
In vivo, BI 2536 (10mg/kg/every other day; 20 days; i.p.) inhibited tumor growth in the cell-derived xenograft model mice[2]. Combining BI 2536 (10mg/kg; every other day for a total of five doses; i.v.) with alisertib impaired DNA repair capacity and significantly delayed tumor growth in mice[4].
References:
[1] Gohda J, Suzuki K, Liu K, et al. BI-2536 and BI-6727, dual Polo-like kinase/bromodomain inhibitors, effectively reactivate latent HIV-1. Sci Rep. 2018 Feb 23;8(1):3521.
[2] Huo J, Shen Y, Zhang Y, et al. BI 2536 induces gasdermin E-dependent pyroptosis in ovarian cancer. Front Oncol. 2022 Aug 9;12:963928.
[3] Hsieh CH, Yeh HN, Huang CT, et al. BI-2536 Promotes Neuroblastoma Cell Death via Minichromosome Maintenance Complex Components 2 and 10. Pharmaceuticals (Basel). 2021 Dec 28;15(1):37.
[4] Zhang J, Liu X, Hou P, et al. BRCA1 orchestrates the response to BI-2536 and its combination with alisertib in MYC-driven small cell lung cancer. Cell Death Dis. 2024 Jul 31;15(7):551.
[5] Li Z, Yang C, Li X, et al. The dual role of BI 2536, a small-molecule inhibitor that targets PLK1, in induction of apoptosis and attenuation of autophagy in neuroblastoma cells. J Cancer. 2020 Mar 5;11(11):3274-3287.
| Cell experiment [1]: | |
Cell lines | Human ovarian cell line A2780 cell |
Preparation Method | Cells were seeded in a 12-well plate and treated with indicated drugs (DMSO, 0.1μM, 0.5μM, 1.0μM and 2.0μM BI 2536) for 72h. Then cells were washed with PBS, harvested, and fixed with anhydrous ethanol overnight. After washed with PBS, PI/RNase staining was added to suspend cells and incubate for 30min in dark. The cell cycle distribution was determined by flow cytometry. |
Reaction Conditions | 0.1μM, 0.5μM, 1.0μM and 2.0μM; 72h |
Applications | BI 2536 inhibited the proliferation of ovarian cancer cells and induced cell cycle arrest at the G2/M phases. |
| Animal experiment [2]: | |
Animal models | Athymic nu/nu mice |
Preparation Method | A total of 5 × 106 SCLC cells, suspended in a 100μL volume, were mixed with an equal volume of Matrigel and inoculated into the dorsal flank of a 4-6 week-old nu/nu mice. Once the tumors became palpable and measurable, mice were randomized into four groups and treated with either DMSO control, BI 2536 alone, alisertib alone, or a combination of BI 2536 and alisertib. BI 2536 (10mg/kg) was administered via tail vein injection every other day for a total of five doses. Alisertib (20mg/kg) was given orally every other day for a total of five doses. Each animal was tracked individually every other day for tumor growth by external caliper measurements of the protruding subcutaneous tumors. The tumor size was calculated using the following formula: Volume = (length × width2)/2. |
Dosage form | 10mg/kg; every other day for a total of five doses; i.v. |
Applications | Combining BI 2536 with alisertib impaired DNA repair capacity and significantly delayed tumor growth in mice. |
References: | |
| Cas No. | 755038-02-9 | SDF | |
| Synonyms | BI-2536;BI2536 | ||
| Chemical Name | 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | ||
| Canonical SMILES | CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C | ||
| Formula | C28H39N7O3 | M.Wt | 521.67 |
| Solubility | ≥ 13.04 mg/mL in DMSO, ≥ 92.4 mg/mL in EtOH with ultrasonic | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9169 mL | 9.5846 mL | 19.1692 mL |
| 5 mM | 383.4 μL | 1.9169 mL | 3.8338 mL |
| 10 mM | 191.7 μL | 958.5 μL | 1.9169 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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