Biological Activity(Only for Reference)

Description

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.

Targets

BTK	TEC	BLK	BMX	LCK)	ITK
0.755-1.02 nM[1]	1.71-2.29 nM[1]	3.66-4.27 nM[1]	4.42-5.57 nM[1]	5.99-6.92 nM[1]	0.187-0.198 μM[1]

In vitro

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 vivo

Protocol

Kinase Assay:[1]

Kinase Assay

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).

Cell Research:

Cell line
Concerntration
Incubation Time
Method

Animal Research:

Animal Models
Formulation
Dosages
Administration

Chemical Information

CAS No.	1599432-18-4
Formula	C56H80N12O9S
Molecular Weight	1097.37
Storage	Powder,-20°C,2 years;DMSO solution,4°C,2 weeks;DMSO solution,-80°C,6 months

Ibrutinib-biotin

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