CPI-0610 MedChemExpress (MCE)

Product Name	CPI-0610
Synonyms	CPI0160 CPI-0610 Pelabresib BET bromodomain inhibitor (4S)-6-(4-Chlorophenyl)-1-methyl-4H-isoxazolo[5,4-d][2]benzazepine-4-acetamide 2-[6-(4-Chloro-phenyl)-1-Methyl-4H-3-oxa-2,5-diaza-benzo[e]azulen-4-yl]-acetaMide Synonyms CPI0160 CPI-0610 Pelabresib BET bromodomain inhibitor (4S)-6-(4-Chlorophenyl)-1-methyl-4H-isoxazolo[5,4-d][2]benzazepine-4-acetamide 2-[6-(4-Chloro-phenyl)-1-Methyl-4H-3-oxa-2,5-diaza-benzo[e]azulen-4-yl]-acetaMide 4H-Isoxazolo[5,4-d][2]benzazepine-4-acetamide, 6-(4-chlorophenyl)-1-methyl-, (4S)- 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
CAS	1380087-89-7
EINECS
Chemical Formula	C20H16ClN3O2
Molecular Weight	365.81
inchi
Package	10 mM * 1 mL;5 mg;10 mg
Price	Email to quote
Descriptions	Pelabresib Pelabresib MedChemExpress (MCE) HY-12863 1380087-89-7 CPI-0610 99.95% Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Room temperature in continental US Descriptions Pelabresib Pelabresib MedChemExpress (MCE) HY-12863 1380087-89-7 CPI-0610 99.95% Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Room temperature in continental US may vary elsewhere. 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. Pelabresib (0-1500 nM 72 hours Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner[2]. Pelabresib (800 nM 72 hours INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest[2]. Pelabresib (800 nM 72 hours INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours[2]. Pelabresib (30-60 mg/kg oral administration for 28 days MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals[1]. BRD4-BD1 39 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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