Ibrutinib-biotin

Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

Research Areas >> Cancer

IC50: 0.755-1.02 nM (BTK), 1.71-2.29 nM (TEC), 3.66-4.27 nM (BLK), 4.42-5.57 nM (BMX), 5.99-6.92 nM (LCK), 33.8-36.3 nM (Src), 0.187-0.198 μM (ITK),5.34-4.87 μM (JAK3)[1]

Ibrutinib-biotin (Compound 1-5) is a probe that consists of Ibrutinib linked to biotin via a long chain linker. Ibrutinib is a TEC family kinase inhibitor. The TEC kinase family is composed of five members, TEC, BTK (Bruton's Tyrosine Kinase), ITK (interleukin-2-inducible T-cell kinase)/EMT/TSK, BMX and TXK/RLK. The TEC family kinases participate in phosphotyrosine- mediated and phospholipid-mediated signaling systems. Many TEC family proteins are abundantly expressed in hematopoietic tissues, and play important roles in the growth and differentiation processes of blood cells[1].

In this study, assay formats are tested for sensitivity, specificity, range, and to determine most suitable anti BTK Antibody. An aliquot of DOHH2 cell lysate (1 mg/mL) is inhibited with 1 μM Ibrutinib then labeled with probe (1 μM). Negative controls: Untreated DOHH2 and Jurkat cell lysates (l mg/mL) are labeled with probe (1 μM) and Untreated DOHH2 cell lysate. Standard Streptavidin plate (5-pack); Read Buffer T (50 mL), SULFO TAG Goat Anti-mouse (50 μg); SULFO TAG Goat Anti-rabbit (50 μg); SULFO TAG streptavidin (50 ug); MSD Standard Plates; MSD Blocker A; Protease inhibitor cocktail; Positive Control lysates from BTK expressing cell line (DOHH2); Negative Control lysates; Ibrutinib (PCI); probe compound 1-5 (biotinylated probe).

[1]. Betty Y. CHANG, et al. Companion diagnostics for tec family kinase inhibitor therapy. WO 2014059368 A1.

Acalabrutinib | GDC-0853 | Evobrutinib | AVL-292 | (±)-Zanubrutinib | ONO-4059 | BMX-IN-1 | GDC-0834 | SNS-062 | RN486 | LFM-A13 | Vecabrutinib | CGI-1746 | BMS-986195 | CNX-774