ZBC 260 MedChemExpress (MCE)

Product Name	BETd-260
Synonyms	BETd-260
CAS	2093388-62-4
EINECS
Chemical Formula	C43H46N10O6
Molecular Weight	798.89
inchi
Package	1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	BETd-260 BETd-260 MedChemExpress (MCE) HY-101519 2093388-62-4 ZBC 260 99.59% -80°C, protect from light, stored under nitrogen Shipping with dry ice. BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4 Descriptions BETd-260 BETd-260 MedChemExpress (MCE) HY-101519 2093388-62-4 ZBC 260 99.59% -80°C, protect from light, stored under nitrogen Shipping with dry ice. BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4 11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells. BETd-260 (ZBC260 Compound 23) is capable of inducing degradation of BRD2, BRD3, and BRD4 proteins at 30–100 pM in the RS4 11 leukemia cells. BETd-260 shows inhibitory activity against the growth of RS4 11 leukemia cells and MOLM-13 cells with IC50s of 51 pM and 2.2 nM, respectively, and induces apoptosis in both RS4 11 and MOLM-13 cell lines at 3-10 nM[1]. BETd-260 reciprocally modulates the expression of several apoptotic genes in HCC cells, i.e., suppressing the expression of anti-apoptotic Mcl-1, Bcl-2, c-Myc, and XIAP, whereas increasing the expression of pro-apoptotic Bad[2]. BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4 11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4 11 xenograft mice model[1]. Mice[1] To develop xenograft tumors, 5 × 106 RS4 11 cells with 50% Matrigel are injected subcutaneously on the dorsal side of severe combined immunodeficient (SCID) mice, one tumor per mouse. When tumors reach appr 100 mm3, mice are randomly assigned to BETd-260 treatment and vehicle control groups. Animals are monitored daily for any signs of toxicity and weighed 2-3 times per week during the treatment and weighed at least weekly after BETd-260 treatment end. Tumor size is measured 2-3 times per week by electronic calipers during the treatment period and at least weekly after the treatment is end. Tumor volume is calculated as V = LW2/2, where L is the length and W is the width of the tumor[1]. In cell growth experiments, cells are seeded in 96-well cell culture plates at a density of 10000−20000 cells/well in 100 μL of culture medium. BETd-260 is serially diluted in the appropriate medium, and 100 μL of the diluted solution containing BETd-260 is added to the appropriate wells of the cell plate. After addition of BETd-260, the cells are incubated for 4 days at 37°C in an atmosphere of 5% CO2. Cell growth is evaluated by a lactate dehydrogenase-based WST-8 assay using a multimode microplate reader. The WST-8 reagent is added to the plate, incubated for at least 1 h, and read at 450 nm. The readings are normalized to the DMSO-treated cells, and the IC50 is calculated by nonlinear regression analysis using GraphPad Prism 6 software[1]. BRD4 50) BRD2 30-100 pM (IC50) BRD3 30-100 pM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25 61(2):462-481. [Content Brief] [2]. Zhang H, et al. Targeting BET Proteins With a PROTAC Molecule Elicits Potent Anticancer Activity in HCC Cells. Front Oncol. 2020 9:1471. Published 2020 Jan 14. [Content Brief]
Supplier Website	https://www.medchemexpress.com/BETd-260.html
Last Update	2025-05-21 16:50:25

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