1808160-52-2
1808160-52-2 structure
- Name: BET inhibitor CF53
- Chemical Name: CF53
- CAS Number: 1808160-52-2
- Molecular Formula: C24H25N7O2
- Molecular Weight: 443.50
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2019-02-11 17:38:37
- Modify Date: 2024-01-02 17:11:53
-
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds 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, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].
| Name | CF53 |
|---|
| Description | CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds 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, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1]. |
|---|---|
| Related Catalog | |
| Target |
BRD4 (BD1):<1 nM (Ki) BRD4 (BD1):2 nM (IC50) BRD4 (BD1):2.2 nM (Kd) BRD4 (BD2):0.8 nM (Kd) BRD2 (BD2):0.6 nM (Kd) BRD2 (BD1):1.1 nM (Kd) BRD3 (BD2):0.49 nM (Kd) BRD3 (BD1):0.52 nM (Kd) BRDT (BD2):1 nM (Kd) BRDT (BD1):2 nM (Kd) CREBBP:47 nM (Kd) EP300:110 nM (Kd) CECR2:570 nM (Kd) |
| In Vitro | CF53 (Compound 28) is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1, very selective over non-BET bromodomain-containing proteins. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds 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[1]. CF53 exhibits potent anti-tumor activity, with IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively[1]. |
| 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[1]. |
| References |
| Molecular Formula | C24H25N7O2 |
|---|---|
| Molecular Weight | 443.50 |
| Storage condition | 2-8℃ |