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dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity. dBET6 is a highly potent, selective and cell-permeable degrader of BET, which has antitumor activity. dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4.
In vivo, dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL.
| Molecular Weight | 841.37 |
| Formula | C42H45ClN8O7S |
| CAS Number | 1950634-92-0 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage | Powder -20°C |
| Related PROTAC Products |
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ARV-393 is an orally active PROTAC degrader targeting BCL6 for studies related to diffuse large B-cell lymphoma. ARV-393 utilizes the ubiquitin-proteasome system to target the degradation of BCL6. |
| ARV-766
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations. ARV-766 has the potential to be first- and best-in class PROTAC AR degrader in mCRPC. |
| Indisulam
Indisulam is a carbonic anhydrase inibitor and antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition. |
| A1874
A1874 is a BRD4-degrading PROTAC which inhibits many cancer cell lines proliferation, with DC50 of 32 nM (induce BRD4 degradation in cells). |
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