other

Ibrutinib (PCI-32765)

MBS575412

10 mg

135 USD

Inhibitor

Ibrutinib (PCI-32765)

[Ibrutinib]

0.98

2 Years -80°C in solvent. 3 years -20°C powder.

Structure

CAS: 936563-96-1. Formula: C25H24N6O2. Solubility: DMSO: 82 mg/mL (186.2 mM). Ethanol: <1 mg/ml. Water: <1 mg/ml. Receptor (IC50): BLK: 0.5 nM (cell free). Bmx: 0.8 nM (cell free). BTK: 0.5 nM (cell free). CSK: 2.3 nM (cell free). FGR: 2.3 nM (cell free). BRK: 3.3 nM (cell free)

Kinase Assay: In vitro kinase IC50s were measured using 33P filtration binding assay after 1 h incubation of kinase, 33P-ATP, inhibitor, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays were performed at Reaction Biology [1]. Cell Assay: CD20+ B and CD3+ T cells were purified by negative selection (RosetteSep, >90% purity) from buffy coat PBMCs and viably frozen in 10% DMSO. Cells were thawed at 37 degree C and maintained in growth media (RPMI media containing 10% FCS). B cells were stimulated with goat anti-human IgM F(ab?)2 (10 ug/mL) and T cells were stimulated with anti-CD3/CD28 coated beads ata 1:1 bead/cell ratio. Cells were stained with PE-CD69 and analyzed by flow cytometry, gating on viable lymphocytes. PCI-32765 at concentrations lower than 10 uM did not decrease B- or T-cell viability during the course of the experiment, although PCI-32765 did block the modest survival benefit of anti-IgM stimulation in B cells. For washout experiments, cells were rinsed three times in 10 volumes of growth media, a protocol that was confirmed to completely wash away inhibition of BCR signaling by PCI-29732, a reversible Btk inhibitor [1]. Cell line: Chronic lymphocytic leukemia (CLL) cells. Animal Experiment: Animal Model: MRL-Fas(lpr) lupus model and collagen-induced arthritis model.

MBS575412 (Ibrutinib is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK HCK, less potent to EGFR, Yes , ErbB2, JAK3, etc.

440.50

10 mg

135 USD

1ml/10mM (in DMSO)

145

50 mg

155

100 mg

170

200 mg

190