N-piperidine Ibrutinib hydrochloride |
| Katalog-Nr.GC62255 |
N-Piperidin-Ibrutinib-Hydrochlorid (Verbindung 1) ist ein reversibles Ibrutinib-Derivat. N-Piperidin-Ibrutinib-Hydrochlorid ist ein potenter BTK-Inhibitor mit IC50-Werten von 51,0 und 30,7 nM fÜr WT-BTK bzw. C481S-BTK. N-Piperidin-Ibrutinib-Hydrochlorid kann als BTK-Ligand bei der Synthese einer Reihe von PROTACs wie SJF620 verwendet werden. SJF620 ist ein potenter PROTAC BTK Abbauer mit einem DC50 von 7,9 nM.
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Cas No.: 2231747-18-3
Sample solution is provided at 25 µL, 10mM.
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N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively[1]. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 . SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM[2].
N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs. SJF638, SJF678, and SJF608 are potent PROTAC BTK degraders with DC50s of 374, 162, and 8.3 nM, respectively[2].
[1]. Buhimschi AD, et al. Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation. Biochemistry. 2018 Jul 3;57(26):3564-3575. [2]. Jaime-Figueroa S, et al. Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. Bioorg Med Chem Lett. 2020 Feb 1;30(3):126877.
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