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MT-802 is a potent BTK degrader based on PROTAC technology, it induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 degrades BTK with a DC50 of 9.1 nM with maximal degradation being observed by 250 nM. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL).
| Molecular Weight | 787.82 |
| Formula | C41H41N9O8 |
| CAS Number | 2231744-29-7 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PROTAC Products |
|---|
| CR8
CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). |
| ARV-393
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. |
| dBET6
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. |
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