AZD-8835

SKU: orb1300479

Description

AZD-8835

Research Area

Signal Transduction

Key Properties

• CAS Number: 1620576-64-8
• MW: 469.54
• Purity: 98.49%
• 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 administratio [1.
• 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.
• 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