N-piperidine Ibrutinib hydrochloride |
| カタログ番号GC62255 |
N-ピペリジン イブルチニブ塩酸塩 (化合物 1) は、可逆的なイブルチニブ誘導体です。 N-ピペリジン イブルチニブ塩酸塩は、WT BTK および C481S BTK の IC50 がそれぞれ 51.0 および 30.7 nM の強力な BTK 阻害剤です。 N-ピペリジン イブルチニブ塩酸塩は、SJF620 などの一連の PROTAC の合成において BTK リガンドとして使用できます。 SJF620 は、DC50 が 7.9 nM の強力な PROTAC BTK 分解剤です。
Products are for research use only. Not for human use. We do not sell to patients.
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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