For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I046372 |
| CAS Number | 1380087-89-7 |
| Synonyms | 2-[(4S)-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide |
| Molecular Formula | C20H16ClN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H16ClN3O2/c1-11-18-14-4-2-3-5-15(14)19(12-6-8-13(21)9-7-12)23-16(10-17(22)25)20(18)26-24-11/h2-9,16H,10H2,1H3,(H2,22,25)/t16-/m0/s1 |
| InChIKey | GCWIQUVXWZWCLE-INIZCTEOSA-N |
| SMILES | CC1=NOC2=C1C3=CC=CC=C3C(=NC2CC(=O)N)C4=CC=C(C=C4)Cl |
| Reference | [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. |
