AZD-8835

SKU: orb1300479

Description

AZD-8835 is a potent and selective mixed inhibitor of PI3Kα and PI3Kδ isoforms, with significantly lower activity against PI3Kβ and PI3Kγ. This compound is a valuable research tool for investigating PI3K signaling in oncology and immunology, supporting both in vitro biochemical assays and in vivo disease model studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1620576-64-8
• MW: 469.54
• Purity: 99.88% (May vary between batches)
• Formula: C₂₂H₃₁N₉O₃
• SMILES: CCn1nc(nc1-c1cnc(N)c(n1)-c1nnc(o1)C(C)(C)C)C1CCN(CC1)C(=O)CCO
• Target: PI3K
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.13 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:86 mg/mL (183.16 mM)

Bioactivity

• Target IC50:
  PI3Kγ:90 nM|PI3Kα:6.2 nM|PI3Kα (E542K):6 nM|PI3Kβ:431 nM|PI3Kδ:5.7 nM|PI3Kα (H1047R):5.8 nM
• In Vivo:
  AZD8835 has antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously and displays high metabolic stability and suitable physical properties for oral administration.
• In Vitro:
  AZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H1047R mutations) and PI3Kδ with excellent selectivity vs. PI3Kβ, PI3Kγ and an excellent general kinase selectivity. AZD8835 is a potent inhibitor of p-Akt in cells sensitive to PI3Kα inhibition (IC50=0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50=0.049 μM in JeKo-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50=3.5 μM in PTEN null breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line).
• Cell Research:
  BT474, MCF7, or T47D cells are seeded in 384-well plates at a density of 500 to 2,000 cells per well and incubated overnight. Cells are dosed with compound(s) and cell confluency is measured at 4-hour intervals over several days.(Only for Reference)

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

PI3Kβ, PI3Kδ, PI3Kγ, PI3K, PI3Kα, Phosphoinositide 3-kinase, AZD8835, AZD-8835, AZD 8835, inhibit, Inhibitor

Compound Identifiers

PubChem CID

76685059