Pelabresib
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].
Product Specifications
CAS Number
[1380087-89-7]
Product Name Alternative
CPI-0610
UNSPSC
12352005
Target
Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Epigenetics
Applications
Cancer-programmed cell death
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 Formula
C20H16ClN3O2
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)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
BRD4
Available Sizes
Curated Selection
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