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Chemical Structure : BET inhibitor CF53
CAS No.: 1808160-52-2
Catalog No.: PC-35401Not For Human Use, Lab Use Only.
BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).
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|---|---|---|---|
| 5 mg | $278 | In stock | |
| 10 mg | $428 | In stock | |
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| 100 mg | Get quote |
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BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).
BET inhibitor CF53 potently inhibits different BET proteins with Kd values of 0.5-2.2 nM, weakly inhibits CREBBP (Ki=47 nM) and shows excellent selectivity over other bromodomain containing proteins.
BET inhibitor CF53 inhibits cell growth in MOLM-13 and MDA-MB-231 cell lines with IC50 of 7 and 85 nM, respectively.
CF53 demonstrates significant antitumor activity in both triple-negative breast cancer and acute leukemia xenograft models in mice.
| M.Wt | 443.511 | |
| Formula | C24H25N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(3-Cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amine |
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1. Zhao Y, et al. J Med Chem. 2018 Jul 17. doi: 10.1021/acs.jmedchem.8b00483.
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