| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C46H49ClN10O3 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibitor, degrades BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. Its antitumor activity depends on BET degradation and can be attenuated by Pomalidomide, a CRBN binding molecule, and it induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research[1][2]. It has a molecular formula of C46H49ClN10O3 and a molecular weight of 825.40 g/mol.
Physical & Chemical Properties
| CAS Number | 2154350-81-7 |
|---|---|
| Molecular Formula | C46H49ClN10O3 |
| Molecular Weight | 825.40 g/mol |
| 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 |
| Target | BRD4 |
| Signaling Pathway | PROTAC; Epigenetics |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
BRD4 4.3 nM (DC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
CFT-743 binds tightly to purified BRD4 BD1 and to purified CRBN-DDB1 complex, and the two proteins show minimal cooperative effects during ternary complex formation[1]. High-affinity ternary complex formation between purified BRD4 BD1 and purified CRBN-DDB1 is driven by CFT-743, with minimal protein-protein cooperativity in the complex[1]. In HeLa cell-free lysates, CFT-743 (3-1000 nM; 30-90 min) causes low-rate ubiquitination of purified HA-tagged BRD4 BD1, showing tight BD1 binding and moderate CRBN binding, in line with an essential activator kinetic model[1]. In 293T cells, CFT-743 (3 h; 10 μM down through serial half-log dilutions) causes minimal degradation of HiBiT-tagged BRD4 BD1, with a DC50 of 4.3 nM and very low maximal efficacy[1]. In HeLa cell-free lysates, CFT-743 (30-3000 nM; 30-90 min) induces low-rate ubiquitination of endogenous BRD4, with a slower maximal velocity than for purified BRD4 BD1 because the endogenous target concentration is lower[1]. In HeLa cell-free lysates, CFT-743 preferentially induces diubiquitination of purified HA-tagged BRD4 BD1, in contrast to other tested BiDACs, which mainly induce monoubiquitination[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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