Structure of BI 2536
CAS No.: 755038-02-9
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BI 2536 is a dual inhibitor of PLK1 and BRD4, with IC50s of 0.83 nM and 25 nM, respectively. BI-2536 also suppresses IFNB gene transcription.
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CAS No. : | 755038-02-9 |
Formula : | C28H39N7O3 |
M.W : | 521.65 |
SMILES Code : | O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(C4CCCC4)[C@@H]5CC)=NC=C3N(C)C5=O)C(OC)=C2 |
MDL No. : | MFCD10565924 |
InChI Key : | XQVVPGYIWAGRNI-JOCHJYFZSA-N |
Pubchem ID : | 11364421 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HeLa cells | 0.1 μM | 45 min | To study the effect of PLK1 inhibitor on HeLa cells, observed downregulation of PLK1 substrates and upregulation of ATM and ATR substrates. | PMC9876800 |
hESPL1flox/Δ cells | 25 or 200 nM | 3 h | To test the critical role of Plk1 in the cell cycle, it was found that Plk1 activity in late G2 or early M phase is essential for centriole disengagement and duplication | PMC2746921 |
SUM-149 cells | 25 nM | 7 days | Inhibited PLK1 activity, significantly reduced cell viability | PMC4304881 |
SUM-149 cells | 25 nM | 7 days | To evaluate the inhibitory effect of BI 2536 on PLK1 and its impact on cell growth, results showed that SUM-149 cells were more sensitive to BI 2536 than MCF-10A cells. | PMC4304881 |
bone marrow-derived dendritic cells (BMDCs) | 1 μM | 2 or 4 h | BI 2536 specifically abrogates transcription of antiviral genes without affecting inflammatory genes following stimulation with LPS, poly(I:C), or Pam3CSK4. | PMC3809888 |
HeLa cells | 250 nM | 2 h | Inhibit PLK1 activity and observe cell behavior in prometaphase | PMC4206221 |
Human pulmonary arterial smooth muscle cells (hPASMCs) | 50 nM | 24 h | To investigate the effect of BI 2536 on apoptosis in hPASMCs, results showed that BI 2536 significantly induced apoptosis in hPASMCs. | PMC10440037 |
LNCaP cells | 10 nM - 100 nM | 24 h | To investigate the effects of BI 2536 on LNCaP cells, results showed that Pim1-overexpressing cells were more sensitive to the inhibitory effects of BI 2536, exhibiting more mitotic arrest and apoptosis. | PMC4086184 |
Patched mutant tumor cells | 0.15 nM - 1.5 μM | 48 hours | To evaluate the inhibitory effect of CCT129202 on tumor cell proliferation, results showed significant inhibition of tumor cell proliferation. | PMC3800039 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
mice | VSV infection model | intravenously | 500 μg | 3 hours before and 2 hours after infection | BI 2536 inhibits antiviral cytokine mRNA production, while increasing viral replication during in vivo VSV infection. | PMC3809888 |
Mice | Hypoxia-induced pulmonary hypertension model | Tail vein injection | 50 mg/kg | Once per week for 4 weeks | To investigate the therapeutic effect of BI 2536 on hypoxia-induced pulmonary hypertension, results showed that BI 2536 significantly reduced right ventricular systolic pressure (RVSP) and right ventricular hypertrophy (RV/LV + S). | PMC10440037 |
nude mice | Pim1-overexpressing prostate cancer xenograft model | intravenous injection | 25 mg/kg | twice a week for three weeks | To investigate the effects of BI 2536 on Pim1-overexpressing prostate cancer xenograft models, results showed that BI 2536 dramatically inhibited the growth of Pim1-overexpressing tumors and induced more mitotic arrest and apoptosis. | PMC4086184 |
Nude mice | LS174T colon cancer cell xenograft model | Gavage | 30 mg/kg twice a week | Twice a week, for 11 days | Synergistically inhibited tumor growth | PMC8492540 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT00526149 | Breast Cancer ... More >> Endometrial Cancer Head and Neck Cancer Melanoma (Skin) Ovarian Cancer Sarcoma Less << | Phase 2 | Completed | - | Belgium ... More >> U.Z. Gasthuisberg Leuven, Belgium, B-3000 Less << |
NCT00710710 | Pancreatic Neoplasms | PHASE2 | COMPLETED | 2008-10-14 | 1216.10.43001 Boehringer Ingel... More >>heim Investigational Site, Wien, Austria|1216.10.49013 Boehringer Ingelheim Investigational Site, Celle, Germany|1216.10.49009 Boehringer Ingelheim Investigational Site, Düsseldorf, Germany|1216.10.49007 Boehringer Ingelheim Investigational Site, Essen, Germany|1216.10.49001 Boehringer Ingelheim Investigational Site, Freiburg/Breisgau, Germany|1216.10.49005 Boehringer Ingelheim Investigational Site, Hamburg, Germany|1216.10.49010 Boehringer Ingelheim Investigational Site, Herne, Germany|1216.10.49008 Boehringer Ingelheim Investigational Site, München, Germany|1216.10.49003 Boehringer Ingelheim Investigational Site, Stuttgart, Germany|1216.10.49002 Boehringer Ingelheim Investigational Site, Ulm, Germany Less << |
NCT00412880 | Carcinoma, Small Cell | PHASE2 | COMPLETED | 2008-06-30 | 1216.11.007 Boehringer Ingelhe... More >>im Investigational Site, Fayetteville, Arkansas, United States|1216.11.003 Boehringer Ingelheim Investigational Site, Chicago, Illinois, United States|1216.11.006 Boehringer Ingelheim Investigational Site, Evanston, Illinois, United States|1216.11.002 Boehringer Ingelheim Investigational Site, Boston, Massachusetts, United States|1216.11.005 Boehringer Ingelheim Investigational Site, Saint Louis, Missouri, United States|1216.11.001 Boehringer Ingelheim Investigational Site, Chapel Hill, North Carolina, United States|1216.11.011 Boehringer Ingelheim Investigational Site, Charleston, South Carolina, United States|1216.11.010 Boehringer Ingelheim Investigational Site, Greenville, South Carolina, United States|1216.11.012 Boehringer Ingelheim Investigational Site, Seattle, Washington, United States|1216.11.009 Alberta Cancer Board, Edmonton, Alberta, Canada Less << |
NCT00243087 | Lymphoma | PHASE1 | COMPLETED | - | Lombardi Comprehensive Cancer ... More >>Center at Georgetown University Medical Center, Washington, District of Columbia, 20007, United States|UNMC Eppley Cancer Center at the University of Nebraska Medical Center, Omaha, Nebraska, 68198-6805, United States|James P. Wilmot Cancer Center at University of Rochester Medical Center, Rochester, New York, 14642, United States|M. D. Anderson Cancer Center at University of Texas, Houston, Texas, 77030-4009, United States Less << |
NCT00706498 | Prostatic Neoplasms | PHASE2 | COMPLETED | - | 1216.19.4407 Boehringer Ingelh... More >>eim Investigational Site, Cambridge, United Kingdom|1216.19.4405 Boehringer Ingelheim Investigational Site, Guildford, United Kingdom|1216.19.4402 Boehringer Ingelheim Investigational Site, Headington, United Kingdom|1216.19.4406 The Christie NHS Foundation Trust, Manchester, United Kingdom|1216.19.4404 Boehringer Ingelheim Investigational Site, Newcastle Upon Tyne, United Kingdom|1216.19.4401 Boehringer Ingelheim Investigational Site, Sutton, United Kingdom Less << |
NCT02215044 | Pancreatic Neoplasms | Phase 1 | Terminated | - | - |
NCT02211859 | Neoplasms | PHASE1 | COMPLETED | - | - |
NCT00701766 | Leukemia, Myeloid, Acute | PHASE2 | COMPLETED | - | 1216.20.43001 Boehringer Ingel... More >>heim Investigational Site, Innsbruck, Austria|1216.20.43002 Boehringer Ingelheim Investigational Site, Wien, Austria|1216.20.49006 Boehringer Ingelheim Investigational Site, Bonn, Germany|1216.20.49002 Boehringer Ingelheim Investigational Site, Frankfurt, Germany|1216.20.49003 Boehringer Ingelheim Investigational Site, Freiburg, Germany|1216.20.49004 Boehringer Ingelheim Investigational Site, Hannover-Heideviertel, Germany|1216.20.49007 Boehringer Ingelheim Investigational Site, Heidelberg, Germany|1216.20.49005 Boehringer Ingelheim Investigational Site, Münster, Germany|1216.20.49001 Boehringer Ingelheim Investigational Site, Ulm, Germany Less << |
NCT00376623 | Carcinoma, Non-Small-Cell Lung | PHASE2 | COMPLETED | 2008-04-01 | 1216.9.49002 Boehringer Ingelh... More >>eim Investigational Site, Freiburg, Germany|1216.9.49007 Boehringer Ingelheim Investigational Site, Gauting, Germany|1216.9.49008 Boehringer Ingelheim Investigational Site, Gro?hansdorf, Germany|1216.9.49001 Boehringer Ingelheim Investigational Site, Heidelberg, Germany|1216.9.49004 Boehringer Ingelheim Investigational Site, Mainz, Germany|1216.9.49005 Boehringer Ingelheim Investigational Site, Mainz, Germany|1216.9.49003 Boehringer Ingelheim Investigational Site, Wiesbaden, Germany Less << |
NCT02211872 | Neoplasms | Phase 1 | Completed | - | - |
NCT02211833 | Carcinoma, Non-Small-Cell Lung | Phase 1 | Completed | - | - |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.92mL 0.38mL 0.19mL |
9.58mL 1.92mL 0.96mL |
19.17mL 3.83mL 1.92mL |
Tags: BI 2536 | BI2536 | BI-2536 | Polo-like Kinase (PLK) | Epigenetic Reader Domain | Apoptosis | PLK1 inhibitor | mitotic arrest | apoptosis | HeLa cells | IC50 | polo-like kinase 1 | 755038-02-9
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P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
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H303 | May be harmful if swallowed |
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H305 | May be harmful if swallowed and enters airways |
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H311 | Toxic in contact with skin |
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H314 | Causes severe skin burns and eye damage |
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H319 | Causes serious eye irritation |
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H335 | May cause respiratory irritation |
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H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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