2154353-03-2
2154353-03-2
Chemical Structure
CFT-1297
- CAS No.: 2154353-03-2
- Formula:C47H50ClN9O3
- Molecular Weight:824.41
InChIKey: SDKKICDYRHTFNX-UHFFFAOYSA-N
SMILES: CC1=NN=C2N1C3=C(C(C4=CC=C(C=C4)Cl)=NC25CC5)C=C(C=C3)C6=CN(N=C6)CCCCCCCN7CCC(CC7)C8=CC=CC9=C8CN(C9=O)C%10CCC(NC%10=O)=O
Biological Activity: CFT-1297 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50 of 5 nM; it has KD values of 2.1 μM, 0.68 μM and 58 nM for CRBN, BRD4 (BD2) and BRD4 (BD1), respectively. CFT-1297 binds weakly to CRBN-DDB1, with a KD value of 2.1 μM[1][2].
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CFT-1297 | 96.06% | CFT-1297 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50 of 5 nM; it has KD values of 2.1 μM, 0.68 μM and 58 nM for CRBN, BRD4 (BD2) and BRD4 (BD1), respectively. CFT-1297 binds weakly to CRBN-DDB1, with a KD value of 2.1 μM. | ||||||||||||||||||||
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References
- [1]. Kroupova A, et al. Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders. Nature communications. 2024 Oct 15;15(1):8885. [Content Brief]
- [2]. Eron SJ, et al. Structural Characterization of Degrader-Induced Ternary Complexes Using Hydrogen-Deuterium Exchange Mass Spectrometry and Computational Modeling: Implications for Structure-Based Design. ACS chemical biology. 2021 Nov 19;16(11):2228-2243.
Keywords
