Description
| Description | BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines. |
| Targets&IC50 | BRD4:<30 pM, BRD2:30-100 pM, BRD:0.0022 μM, BRD3:30-100 pM |
| In vitro | betd – 260 (ZBC260; Compound 23) induced the degradation of BRD2, BRD3 and BRD4 proteins. BETd-260 acted on RS4; The ic50 measured for 11 leukemic cells was 51 pM. The ic50 of BETd-260 in MOLM-13 cells was 2.2 nM. BETd-260 at 3-10 nM could induce RS4; 11 and MOLM-13 cell apoptosis. Moreover, BETd-260 inhibited the transcription and translation of anti-apoptotic genes Mcl-1, Bcl-2, c-Myc and XIAP and increased the transcription and translation of pro-apoptotic gene Bad in HCC cells[1]. |
| In vivo | 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]. 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. |
| Synonyms | ZBC 260 |
| Molecular Weight |
798.89 |
| Formula | C43H46N10O6 |
| CAS No. | 2093388-62-4 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 22.5 mg/mL (28.2 mM),
Need ultrasonic
H2O: 0.1 mg/mL,
insoluble
( < 1 mg/ml refers to the product slightly soluble or insoluble )
