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Chemical Structure : QCA570
CAS No.: 2207569-08-0
Catalog No.: PC-35399Not For Human Use, Lab Use Only.
QCA570 is a highly potent efficacious BET degrader (PROTAC) with IC50 of 10 nM (BRD4 BD1).
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QCA570 is a highly potent efficacious BET degrader (PROTAC) with IC50 of 10 nM (BRD4 BD1).
QCA570 effectively induces degradation of BET proteins and inhibits cell growth in human acute leukemia cell lines at pM level; inhibits cell growth in MV4;11, MOLM-13, and RS4;11 cell lines with IC50 values of 8.3, 62, and 32 pM, respectively.
QCA570 is >10-times more potent than ZBC260 (BETd-260, Cat# PC-60102) in the MV4;11 and MOLM-13 cell lines.
QCA570 (10-30 pM) is very effective in reducing the levels of c-Myc protein in the RS4;11 cell line and the MV4;11 cell line.
QCA570 causes complete and durable tumor regression in leukemia xenograft models in mice.
| M.Wt | 695.798 | |
| Formula | C39H33N7O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(4-(5-(4-((3-Benzyl-9-methyl-4H,6H-thieno[2,3-e][1,2,4]-triazolo[3,4-c][1,4]oxazepin-2-yl)ethynyl)-1H-pyrazol-1-yl)pent-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione |
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1. Qin C, et al. J Med Chem. 2018 Jul 18. doi: 10.1021/acs.jmedchem.8b00506.
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