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AZD-8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | 40 € | In Stock | |
10 mg | 59 € | In Stock | |
25 mg | 113 € | In Stock | |
50 mg | 164 € | In Stock | |
100 mg | 301 € | In Stock | |
1 mL x 10 mM (in DMSO) | 49 € | In Stock |
Description | AZD-8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM). |
Targets&IC50 | PI3Kα:6.2 nM, PI3Kδ:5.7 nM |
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)[2]. |
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[1][2]. |
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) |
Alias | AZD8835 |
Molecular Weight | 469.54 |
Formula | C22H31N9O3 |
Cas No. | 1620576-64-8 |
Smiles | CCn1nc(nc1-c1cnc(N)c(n1)-c1nnc(o1)C(C)(C)C)C1CCN(CC1)C(=O)CCO |
Relative Density. | 1.45 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 86 mg/mL (183.2 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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