CNX-774

SKU: orb1223394

Description

CNX-774 is a potent Btk inhibitor (IC50 < 1 nM). Recently Bruton's tyrosine kinase (BTK) , a crucial terminal kinase enzyme in the B-cell antigen receptor (BCR) signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders.

Key Properties

• CAS Number: 1202759-32-7
• MW: 499.5
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₂FN₇O₃
• SMILES: c1c(ccc(c1)Oc1ccnc(c1)C(=O)NC)Nc1nc(c(cn1)F)Nc1cccc(c1)NC(=O)C=C
• Target: Apoptosis
• Solubility: DMSO : ≥ 45 mg/mL. 90.09 mM

Bioactivity

• In Vivo:
  CNX-774 is stable and non-reactive in fresh human and rat whole blood and does not covalently bond to any of the mid-level abundance human plasma proteins. CNX-774 demonstrates potent inhibitory activity towards the intended target, Btk, while achieving remarkable specificity in a variety of assays designed to assess off-target reactivity towards abundant cellular thiols and blood proteins.
• In Vitro:
  CNX-774 strongly inhibits Btk activity in Ramos cells with an IC50 of 1-10 nM. CNX-774 demonstrates strong time- and dose-dependent occupancy of Btk in Ramos cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CNX774 | CNX 774 | CNX-774

Quick Database Links

Gene Symbol

Apoptosis