Entospletinib

SKU: orb1301072

Description

Entospletinib (GS-9973) is a potent and selective oral inhibitor of spleen tyrosine kinase (Syk) with an IC50 of 7.7 nM. It is a research tool for investigating hematological cancers and autoimmune disorders, showing activity in both cellular assays and animal models of disease.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1229208-44-9
• MW: 411.46
• Purity: 99.74% (May vary between batches)
• Formula: C₂₃H₂₁N₇O
• SMILES: C1CN(CCO1)c1ccc(Nc2nc(cn3ccnc23)-c2ccc3cn[nH]c3c2)cc1
• Target: Syk
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (6.08 mM);DMSO:50 mg/mL (121.52 mM)

Bioactivity

• Target IC50:
  MV-4-11 cells:327 nM (EC50)|Ramos cells:2 nM (EC50)|TF-1 cells:453 nM (EC50)|Syk:7.7 nM|Bone marrow cells:582 nM|HUVECs:> 1000 nM (EC50)
• In Vivo:
  METHODS: To investigate the anti-inflammatory activity of Entospletinib, Entospletinib (100 mg/kg) was administered orally twice daily to K/BxN serum-induced arthritis mice. RESULTS: Entospletinib significantly reduced macroscopic manifestations of joint inflammation, including joint swelling and clinical scores. METHODS: To study the anti-inflammatory activity of Entospletinib, Entospletinib (10 mg/kg) was administered orally to a rat CIA model. RESULTS: Entospletinib showed significant anti-inflammatory effect.
• In Vitro:
  METHODS: NALM-6 and SEM cell lines were treated with Entospletinib (1, 5, and 10 μM) for 72 hours, and the expression levels of target proteins were detected using Western Blot. RESULTS: The expressions of key proteins including pAKT, pERK, pGSK3β, p53 and BCL-6 were significantly affected by Entospletinib.
• Cell Research:
  In MV-4-11 cells, the functional effect of the compound on the cellular Flt3 activity was determined by inhibition of cell proliferation. Cells were diluted in 96 well flat bottom tissue culture plates in RPMI medium containing 10% FBS and compound dilutions were added and incubated at 37°C for 72 hours. Aramazol (10%) was added to the cells and the cells were incubated for another 12-18 hours at 37°C. Finally, the inhibition of the relative cell number was measured at 570/600 nm in the spectrophotometer.
• Animal Research:
  In the rat collagen-induced arthritis (CIA) model, Entospletinib (10 mg/kg), which is dissolved in hydrogenated castor oil,ethanol or physiological saline, is taken by oral.

Storage & Handling

• Storage: keep away from direct sunlight,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

inhibit, Inhibitor, Entospletinib, GS 9973, GS9973, GS-9973, Syk, Spleen tyrosine kinase

Compound Identifiers

PubChem CID

59473233