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Pelabresib

Product Specifications

Product Name Alternative

CPI-0610

UNSPSC Description

Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC[1].

Target Antigen

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CPI-0610.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3C4=C1ON=C4C

Molecular Weight

365.81

References & Citations

[1]Albrecht BK, et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem. 2016 Feb 25;59(4):1330-9.|[2]Siu KT, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Aug;31(8):1760-1769.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-12863/Pelabresib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-12863/Pelabresib-SDS-MedChemExpress.pdf

Clinical Information

Phase 3

CAS Number

1380087-89-7

Available Sizes

Curated Selection

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