CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K i of In Vitro CF53 (Compound 28) binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, K d s are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively. CF53 exhibits IC 50 s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CF53 (25, 50 mg/kg, p.o.) exhibits potent anti-tumor activity both in MDA-MB-231 xenograft tumor model and in RS4;11 model in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:BRD4 (BD1)
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CF53
CAS number:1808160-52-2 molecular formula:C24H25N7O2
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Specs
| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1808160-52-2 | molecular formula | C24H25N7O2 |
| molecular weight | 443.50 g/mol | Exact mass | ≥99% |
| PSA | 107.000 Ų | logp | 4.300 |
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