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Chemical Structure| 1628607-64-6 Chemical Structure| 1628607-64-6

Structure of INCB054329
CAS No.: 1628607-64-6

Chemical Structure| 1628607-64-6

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INCB054329 is a potent and selective BET protein inhibitor that targets BD1 and BD2 of BRD2, BRD3 and BRD4.

Synonyms: INCB054329

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Product Details of INCB054329

CAS No. :1628607-64-6
Formula : C19H16N4O3
M.W : 348.36
SMILES Code : O=C1NC2=C3N1[C@@H](C4=NC=CC=C4)COC3=C(C5=C(C)ON=C5C)C=C2
Synonyms :
INCB054329
MDL No. :MFCD31631585

Safety of INCB054329

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of INCB054329

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4-BD1, IC50:119 nM

    BRD3-BD1, IC50:9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
768-O cells 4, 7, 10 µmol/L 36 hours Inhibited RCC cell proliferation and eIF4EBP1 expression PMC7610328
769-P cells 4, 7, 10 µmol/L 36 hours Inhibited RCC cell proliferation and eIF4EBP1 expression PMC7610328
ACHN cells 4, 7, 10 µmol/L 36 hours Inhibited RCC cell proliferation and eIF4EBP1 expression PMC7610328
OVCAR-3 1μM 24 hours INCB054329 alone or in combination with olaparib reduced BRCA1 and RAD51 expression and increased DNA damage and apoptosis markers pH2AX and cleaved PARP. PMC5986599
SKOV-3 1μM 24 hours INCB054329 reduced BRCA1 expression and increased DNA damage and apoptosis markers pH2AX and cleaved PARP. PMC5986599

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice ACHN xenograft model Oral gavage 90 mg/kg/day Once daily for 14 days Inhibited RCC tumor growth and c-myc expression PMC7610328
Nude mice SKOV-3 subcutaneous tumor model Oral 25mg/kg Twice daily for 3 weeks INCB054329 in combination with olaparib significantly inhibited tumor growth, reduced tumor volume and weight, and increased expression of apoptosis and DNA damage markers. PMC5986599

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03896815 - NO_LONGER_AVAILABLE - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.71mL

5.74mL

2.87mL

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
 

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