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Chemical Structure| 1380087-89-7 Chemical Structure| 1380087-89-7

Structure of Pelabresib
CAS No.: 1380087-89-7

Chemical Structure| 1380087-89-7

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CPI-0610 is an inhibitor of BET bromodomains BRD2, BRD3, BRD4, and BRDT via binding to the acetylated lysine recognition motifs.

Synonyms: CPI-0610

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Product Details of Pelabresib

CAS No. :1380087-89-7
Formula : C20H16ClN3O2
M.W : 365.81
SMILES Code : O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3C4=C1ON=C4C
Synonyms :
CPI-0610
MDL No. :MFCD28144505
InChI Key :GCWIQUVXWZWCLE-INIZCTEOSA-N
Pubchem ID :57389999

Safety of Pelabresib

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

Related Pathways of Pelabresib

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4-BD1, IC50:39 nM

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Immunodeficient mice Raji-Burkitt lymphoma subcutaneous xenograft model Oral 30 mg/kg Single dose Pelabresib inhibits MYC expression in a dose-dependent manner, with maximum inhibition (75%) achieved 4 hours postdosing. PMC10010313

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02157636 Multiple Myeloma PHASE1 COMPLETED 2016-11-08 -
NCT05391022 Advanced Malignancies|Solid Tu... More >>mor|Hematological Malignancy Less << PHASE1 COMPLETED 2024-02-29 Gabrail Cancer Center Research... More >>, Canton, Ohio, 44718, United States|Gettysburg Cancer Center, Gettysburg, Pennsylvania, 17325, United States|Start Mountain Region, West Valley City, Utah, 84119, United States|Hight Technology Hospital Medcenter, Batumi, Georgia|K. Eristavi National Center of Experimental and Clinical Surgery, Tbilisi, Georgia|Simon Khechinashvili University Hospital, Tbilisi, Georgia|Barcelona HM Nou Delfos, Barcelona, 08023, Spain|Madrid - FJD, Madrid, 28040, Spain|START CIOCC Hospital HM Sanchinarro, Madrid, Spain|Hospital Universitario Virgen del Rocío, Sevilla, 41013, Spain Less <<
NCT01949883 Lymphoma PHASE1 COMPLETED 2017-12-20 -
NCT02986919 Peripheral Nerve Tumors PHASE2 WITHDRAWN 2018-05-17 University of Texas Southweste... More >>rn Medical Center, Dallas, Texas, 75390, United States Less <<
NCT06401356 Hematologic Malignancy|Solid T... More >>umor|Advanced Malignancies Less << PHASE3 RECRUITING 2029-06-30 Hematologic Malignancy/Stem (D... More >>epartment of Medicine, Division of Hematology/Oncology), Los Angeles, California, 90095-8344, United States|Mayo Clinic (Cancer Clinical Research Office), Jacksonville, Florida, 32224-1865, United States|Northwestern Memorial Hospital (Oncology), Chicago, Illinois, 60611-5957, United States|UMHS - University of Michigan Medical Center (Radiation Oncology), Ann Arbor, Michigan, 48109-5000, United States|Mount Sinai Hospital - Oncology, New York, New York, 10029, United States|Weill Cornell Medicine - New York Presbyterian Hospital (Oncology), New York, New York, 10065, United States|ZNA Cadix-Hematology, Antwerpen, 2020, Belgium|Az St-Jan Brugge-Oostende A.V., Brugge, 8000, Belgium|AOU Careggi (Department of Experimental and Clinical Medicine), Firenze, 50141, Italy|Azienda Ospedaliero - Universitaria Maggiore della Carità (SCDU Ematologia), Novara, 28100, Italy|AO Ospedale di Circolo, PO Varese (Ematologia), Varese, 21100, Italy|Amsterdam UMC location Vumc (Hematology), Amsterdam, 1081 HV, Netherlands|Cardiff and Vale University Health Board - University Hospital Wales (Hematology), Cardiff, CF14 4XW, United Kingdom|Beatson West of Scotland Cancer Centre (Hematology), Glasgow, G12 0YN, United Kingdom|Guys and St Thomas' Hospital - Haematology, London, SE1 9RT, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.67mL

2.73mL

1.37mL

27.34mL

5.47mL

2.73mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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