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Chemical Structure : CRCM5484
Catalog No.: PC-72866Not For Human Use, Lab Use Only.
CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.
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CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.
CRCM5484 displays 475-fold selectivity over its first bromodomain (BRD3-BD2 vs BRD3-BD1).
CRCM5484 demonstrates very low activity in various cell-based assays.
CRCM5484 modulates the anti-leukemic activity in combination with various FDA-approved and/or in-development drugs in a cell- and context-dependent differential manner.
| M.Wt | 509.599 | |
| Formula | C24H23N5O4S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kendall Carrasco, et al. J Med Chem. DOI: 10.1021/acs.jmedchem.1c02168
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