BMS-935177

SKU: orb1707529

Description

BMS-935177 is a potent and reversible inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 of 3 nM. This small molecule is utilized in biochemical and cellular research to investigate BTK-dependent signaling pathways in immunological and oncological contexts, both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1231889-53-4
• MW: 502.56
• Purity: 99.89% (May vary between batches)
• Formula: C₃₁H₂₆N₄O₃
• SMILES: Cc1c(cccc1-n1cnc2ccccc2c1=O)-c1ccc(C(N)=O)c2[nH]c3cc(ccc3c12)C(C)(C)O
• Target: BTK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.57 mM);DMSO:117 mg/mL (232.81 mM)

Bioactivity

• Target IC50:
  BTK:3 nM
• In Vivo:
  BMS-935177(5, 20, and 45 mg/kg) inhibits anti-KLH antibodies of the IgG isotype at day 14, with statistically significant reductions at all doses. In satellite mice, BMS-935177 (5 mg/kg) maintains the plasma concentration above the mouse whole blood BCR-stimulated CD69 IC50 value of 2 μM for only 5 h. BMS-935177(10, 20, and 30 mg/kg) provides dose-dependently reduces both the severity and incidence of clinically evident disease in this rodent model of RA. BMS-935177(10 mg/kg) reduces the disease severity about 40%, and the percentage of animals showing any signs of disease is reduced by a third.
• In Vitro:
  In human Ramos B cells, BMS-935177 inhibits calcium flux with an IC50 of 27 nM. BMS-935177 inhibits CD69 surface expression in peripheral B cells stimulated with antiIgM and anti-IgG. Against IgG-containing immune complexdriven low affinity activating FcγRIIa and FcγRIII end points in peripheral blood mononuclear cells, BMS-935177 effectively inhibits TNFα production (IC50 = 14 nM). BMS-935177 shows mean IC50 values of 550 and 2060 nM in human and mouse whole blood, respectively.

Storage & Handling

• Storage: store at low temperature | 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

BMS935177, BMS-935177, BMS 935177, BTK

Compound Identifiers

PubChem CID

70647728