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Chemical Structure| 1260907-17-2 Chemical Structure| 1260907-17-2

Structure of Molibresib
CAS No.: 1260907-17-2

Chemical Structure| 1260907-17-2

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Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with an IC50 of 32.5-42.5 nM.

Synonyms: I-BET-762; GSK525762; GSK525762A

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Product Details of Molibresib

CAS No. :1260907-17-2
Formula : C22H22ClN5O2
M.W : 423.90
SMILES Code : O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
Synonyms :
I-BET-762; GSK525762; GSK525762A
MDL No. :MFCD22417091
InChI Key :AAAQFGUYHFJNHI-SFHVURJKSA-N
Pubchem ID :46943432

Safety of Molibresib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Molibresib

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BET proteins, IC50:35 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03702036 - - - -
NCT02706535 Drug Interactions Phase 1 Completed - United States, Maryland ... More >> GSK Investigational Site Baltimore, Maryland, United States, 21225 Less <<
NCT03266159 Solid Tumours Phase 2 Withdrawn(Study withdrawn befo... More >>re active to fully evaluate impact of changing practice in target population.) Less << August 19, 2020 -
NCT03150056 Solid Tumours Phase 1 Recruiting July 29, 2019 -
NCT02964507 Neoplasms Phase 2 Recruiting June 1, 2020 -
NCT01587703 Carcinoma, Midline PHASE1 COMPLETED 2019-07-29 GSK Investigational Site, Balt... More >>imore, Maryland, 21231-2410, United States|GSK Investigational Site, Boston, Massachusetts, 02215, United States|GSK Investigational Site, Philadelphia, Pennsylvania, 19104, United States|GSK Investigational Site, Nashville, Tennessee, 37232, United States|GSK Investigational Site, Houston, Texas, 77030, United States|GSK Investigational Site, Clayton, Victoria, 3168, Australia|GSK Investigational Site, Bordeaux Cedex, 33076, France|GSK Investigational Site, Lyon Cedex 08, 69373, France|GSK Investigational Site, Paris Cedex 5, 75248, France|GSK Investigational Site, Seoul, 03080, Korea, Republic of|GSK Investigational Site, Seoul, 03722, Korea, Republic of|GSK Investigational Site, Amsterdam, 1066 CX, Netherlands|GSK Investigational Site, Barcelona, 08035, Spain|GSK Investigational Site, Madrid, 28040, Spain|GSK Investigational Site, Málaga, 29010, Spain|GSK Investigational Site, Sutton, Surrey, SM2 5PT, United Kingdom|GSK Investigational Site, Newcastle upon Tyne, NE7 7DN, United Kingdom Less <<
NCT01943851 Neoplasms PHASE2 COMPLETED 2020-04-30 GSK Investigational Site, Litt... More >>le Rock, Arkansas, 72205, United States|GSK Investigational Site, Aurora, Colorado, 80045, United States|GSK Investigational Site, New York, New York, 10065, United States|GSK Investigational Site, Philadelphia, Pennsylvania, 19104, United States|GSK Investigational Site, Houston, Texas, 77030, United States|GSK Investigational Site, East Melbourne, Victoria, 3002, Australia|GSK Investigational Site, Seoul, 03722, Korea, Republic of|GSK Investigational Site, Seoul, 06351, Korea, Republic of|GSK Investigational Site, Barcelona, 08036, Spain|GSK Investigational Site, Madrid, 28006, Spain|GSK Investigational Site, Madrid, 28040, Spain|GSK Investigational Site, Málaga, 29010, Spain|GSK Investigational Site, Salamanca, 37007, Spain|GSK Investigational Site, Cambridge, CB2 0QQ, United Kingdom|GSK Investigational Site, London, W12 0NN, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL

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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