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Chemical Structure : BETd-246
CAS No.: 2140289-17-2
Catalog No.: PC-60931Not For Human Use, Lab Use Only.
BETd-246 (BETd246) is a potent, second-generation BET protein PROTAC degrader that exhibits superior selectivity, potency and antitumor activity.
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BETd-246 (BETd246) is a potent, second-generation BET protein PROTAC degrader that exhibits superior selectivity, potency and antitumor activity.
BETd-246 completely and selectively depletes BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
BETd-246 displays strong growth inhibition and apoptosis induction activity in TNBC cell lines with IC50 <1 uM, induces a rapid and time-dependent downregulation of MCL1 protein.
BETd-246 decreases BET proteins in xenograft breast tumors and suppress tumor growth in vivo without causing weight loss.
| M.Wt | 946.035 | |
| Formula | C48H55N11O10 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(3-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)propoxy)ethoxy)ethoxy)propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide |
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1. Bai L, et al. Cancer Res. 2017 May 1;77(9):2476-2487.
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