AZD8186

Catalog No.S7694

AZD8186 Chemical Structure

Molecular Weight(MW): 457.47

AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.

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Biological Activity

Description AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.
Targets
PI3Kβ [1]
(Cell-free assay)		 PI3Kδ [1]
(Cell-free assay)		 PI3Kα [1]
(Cell-free assay)
4 nM 12 nM 35 nM
In vitro

AZD8186 potently inhibits p-Akt in MDA-MB-468 cells sensitive to PI3Kβ inhibition and Jeko B cells sensitive to PI3Kδ inhibition with IC50 of 3 nM and 4 nM, respectively. [1] AZD8186 shows preferred growth inhibition activity in most PTEN deficient cell lines with GI50 of <1 μM. [2]
In vivo In nude mice bearing PTEN-deficient PC3 prostate tumor xenografts, AZD8186 (100 mg/kg, p.o.) strongly inhibits Akt phosphorylation levels, and causes significant tumor growth inhibition. When used in combination with ABT, AZD8186 (60 mg/kg, p.o.) results in complete inhibition of tumor growth. [1] In the mouse PTEN-null TNBC models HCC70 and MDA-MB-468, and the prostate models HID28, AZD8186 (50 mg/kg, p.o.) also inhibits the growth of tumors. [2] Combination therapy using AZD8186 with androgen deprivation results in long-lasting tumor regression, which persisted after treatment cessation. [3]

Protocol

Kinase Assay:[1]
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PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ enzyme assays:

The inhibition of PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ human recombinant PI3K isoforms is evaluated using a Kinase-Glo Plus Assay Kit. 12 point half-log concentration-response curves with a top concentration of 100 μM are constructed by dispensing DMSO solubilised compounds into white 384-well medium-binding microplates using an Echo 555. 3 μL of the appropriate PI3K in Tris buffer (50 mM Tris pH7.4, 0.05% CHAPS, 2.1 mM DTT, and 10 mM MgCl2) is added. The plate is covered and allowed to pre-incubate with compound for 20 minutes prior to addition of 3 μL of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 80 minutes by the addition of Kinase Glo detection solution. Plates are covered and incubated for 30 minutes at room temperature before the luminescence signal is read using a PHERAstar plate reader. The final concentrations of DMSO, ATP and PIP2 in the assay are 2%, 8 μM, and 80 μM respectively. The final concentrations of PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ are respectively 20 nM, 20 nM, 45 nM and 30 nM. For PI3Kα, PI3Kβ and PI3Kδ the concentration of active enzyme is determined as outlined in the enzyme assay tight binding limit determination section. For PI3Kγ the concentration of enzyme is determined by Bradford assay. IC50 values are calculated using Genedata Screener.
Cell Research:[2]
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  • Cell lines: A subset of cancer cell lines
  • Concentrations: ~30 μM
  • Incubation Time: 72 hours
  • Method: Cells are seeded in 96-well plates, at a density to allow for logarithmic growth during the 72 hour assay, and incubated overnight at 37°C, 5% CO2. Cells are treated with AZD8186 (30 to 0.003 μM) for 72 hours and cell proliferation measured by MTS. The CellTiter Aqueous Non-Radioactive Cell Proliferation Assay reagent is used in accordance with the manufacturer’s protocol and Absorbance measured with Tecan Ultra instrument. Pre-dose measurements are made and the concentration needed to reduce the growth of treated cells to half that of untreated cells (GI50) values are determined.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Nude mice bearing PTEN-deficient PC3 prostate tumor xenografts
  • Formulation: 10% DMSO / 60% TEG/ 30% WFI
  • Dosages: 100 mg/kg b.i.d
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL warmed (198.92 mM)
Ethanol 35 mg/mL warmed (76.5 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10% DMSO + 60% TEG+ 30% WFI
For best results, use promptly after mixing. 		16mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 457.47
Formula

C24H25F2N3O4
CAS No. 1627494-13-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01884285 Recruiting Advanced Castrate-resistant Prostate Cancer CRPC|Squamous Non-Small Cell Lung Cancer sqNSCLC|Triple Negative Breast Cancer TNBC AstraZeneca July 9 2013 Phase 1
NCT03218826 Recruiting Advanced Malignant Solid Neoplasm|Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Castration-Resistant Prostate Carcinoma|Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Malignant Solid Neoplasm|Metastatic Prostate Carcinoma|PIK3CB Gene Mutation|Progesterone Receptor Negative|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|PTEN Gene Mutation|PTEN Loss|Stage III Prostate Cancer AJCC v8|Stage IIIA Prostate Cancer AJCC v8|Stage IIIB Prostate Cancer AJCC v8|Stage IIIC Prostate Cancer AJCC v8|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8|Triple-Negative Breast Carcinoma|Unresectable Solid Neoplasm National Cancer Institute (NCI) March 16 2018 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID