BIIB068

SKU: orb1298296

Description

BIIB068 is a potent, selective, and orally bioavailable reversible inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 of 1 nM and high kinase selectivity. It is a valuable research tool for investigating BTK's role in B-cell malignancies and autoimmune disorders in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1798787-27-5
• MW: 435.52
• Purity: 98.05%
• Formula: C₂₃H₂₉N₇O₂
• SMILES: CC(C)OC1CN(C1)C(=O)NCc1ccc(cc1C)-c1ccnc(Nc2cnn(C)c2)n1
• Target: BTK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.59 mM);DMSO:30 mg/mL (68.88 mM)

Bioactivity

• Target IC50:
  BTK:0.3 nM (Kd)|BTK:1 nM (IC50)
• In Vivo:
  BIIB068 demonstrated good PK/PD correlation with in vivo EC50 = 0.16 μM based on antibody esponse, similar to in vivo WB pBTK potency in mice. BIIB068 exhibited no adverse effects in the single dose CNS and respiratory studies in rats nor in a single dose cardiovascular study in monkeys. BIIB068 was well tolerated and effective at inhibiting BTK phosphorylation in healthy subjects.
• In Vitro:
  BIIB068 inhibits B cell, neutrophil and monocyte activation in vitro, but not T cell responses.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, FcγR, Inhibitor, anti-IgD, anti-IgM, Autoimmune, Bruton tyrosine kinase, BIIB068, BIIB-068, BIIB 068, Btk, BTK, ADME, ROS, reversible, phosphorylation, TNFα

Compound Identifiers

PubChem CID

118139356