2154350-81-7
Chemical Structure
CFT-743
- CAS No.: 2154350-81-7
- Formula:C46H49ClN10O3
- Molecular Weight:825.40
InChIKey: LPEKKFOJGTZRLY-UHFFFAOYSA-N
SMILES: O=C1C2=C(CN1C3C(NC(CC3)=O)=O)C(NC4CCN(CC4)CCCCCCN5N=CC(C6=CC=C7C(C(C8=CC=C(C=C8)Cl)=NC9(CC9)C%10=NN=C(C)N7%10)=C6)=C5)=CC=C2
Biological Activity: CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research[1][2].
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CFT-743 | CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research. | |||||||||||||||||||||
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- [1]. Vieux EF, et al. A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination. SLAS Discov. 2021;26(4):547-559. [Content Brief]
- [2]. Ladd B, et al. Abstract 1949: In vivo profiling of BET degraders establishes optimal pharmacological properties that showcase distinct biological differences from BET inhibitors. Cancer Res. 2020;80.
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