BETd-260 (ZBC 260) (Synonyms: ZBC 260) |
| Catalog No.GC32791 |
BETd-260 (ZBC 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 (ZBC 260) potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
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Cas No.: 2093388-62-4
Sample solution is provided at 25 µL, 10mM.
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BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM against BRD4 protein in RS4;11 leukemia cell line.
BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM for BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC260; Compound 23) 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 (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].
[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.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 2093388-62-4 | SDF | |
| Synonyms | ZBC 260 | ||
| Canonical SMILES | CCN1N=C(C2CC2)C=C1NC3=NC(C(NCCCCCC4=CC=CC5=C4CN(C6C(NC(CC6)=O)=O)C5=O)=O)=NC7=C3C8=CC(OC)=C(C9=C(C)ON=C9C)C=C8N7 | ||
| Formula | C43H46N10O6 | M.Wt | 798.89 |
| Solubility | DMSO : 25 mg/mL (31.29 mM);Water : < 0.1 mg/mL (insoluble) | Storage | -80°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2517 mL | 6.2587 mL | 12.5174 mL |
| 5 mM | 0.2503 mL | 1.2517 mL | 2.5035 mL |
| 10 mM | 0.1252 mL | 0.6259 mL | 1.2517 mL |
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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