Pelabresib_product_DataBase

Bioactivity

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

Invitro

CPI-0610 (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].CPI-0610 (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest[2].CPI-0610 (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours[2]. 0 --> Pelabresib 相关抗体: Cell Viability Assay[2] Cell Line:

In Vivo

CPI-0610 (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]. Animal Model:

Name

Pelabresib

CAS

1380087-89-7

Formula

C20H16ClN3O2

Molar Mass

365.81

Appearance

固体

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

Pelabresib

CAS: 1380087-89-7 F: C20H16ClN3O2 W: 365.81