Duvelisib

SKU: orb1306832

Description

Duvelisib

Research Area

Signal Transduction

Key Properties

• CAS Number: 1201438-56-3
• MW: 416.86
• Purity: 99.74%
• Formula: C₂₂H₁₇ClN₆O
• SMILES: C[C@H](Nc1ncnc2[nH]cnc12)c1cc2cccc(Cl)c2c(=O)n1-c1ccccc1
• Target: PI3K
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  p110δ:2.5 nM|PI3Kβ:1564 pM(Ki)|PI3Kγ:243 pM(Ki)|p110α:1602 nM|p110γ:27.4 nM|p110β:85 nM|PI3Kδ:23 pM(Ki)
• In Vivo:
  METHODS: We used an Eμ-TCL1 adoptive transfer mouse model of CLL. After Duvelisib (INK1197, IPI-145) (100 mg/kg, once daily, oral, for 21 days), RESULTS Duvelisib (INK1197, IPI-145) significantly reduce the CLL burden (CD19 CD5 B cells) in the peripheral blood of mice; a the same time the total number of CD3 T cells in the mice was also lower, bu the CD4/CD8 ratio was also reduced.
• In Vitro:
  METHODS: Primary mL blasts (AML#2 and AML#5) were treated with Duvelisib (INK1197, IPI-145) (0.1, 0.5, 1 μM) and cultured for 4 hours. They were then incubated with BMSC conditioned medium for 5 minutes. Whole cell extracts were prepared and Western blot analysis was performed for pAKT (s473 and t308) and total AKT, as well as pMAPK and total MAPK. Results Duvelisib (INK1197, IPI-145) inhibited BMSC CM-induced pAKT (s473 and t308) activation at 0.1 μM; Duvelisib (INK1197, IPI-145) blocked blast migration through its inhibitory effect on AKT phosphorylation a the t308 site.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Phosphoinositide 3-kinase, PI3Kβ, PI3Kα, PI3Kγ, PI3Kδ, PI3K, Inhibitor, INK 1197, INK1197, INK-1197, IPI 145, IPI145, IPI-145, inhibit, Duvelisib

Compound Identifiers

PubChem CID

50905713