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Chemical Structure| 755038-02-9 Chemical Structure| 755038-02-9

Structure of BI 2536
CAS No.: 755038-02-9

Chemical Structure| 755038-02-9

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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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Product Details of BI 2536

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

Safety of BI 2536

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of BI 2536

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4, Kd:37 nM

  • PLK2

    PLK2, IC50:3.5 nM

  • PLK3

    PLK3, IC50:9.0 nM

  • PLK1

    PLK1, IC50:0.83 nM

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 - -

Protocol

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

References

 

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