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AZD8186

Catalog No. T6773   CAS 1627494-13-6

AZD8186 is an effective and specific PI3Kβ/δ inhibitor (IC50: 4/12 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
AZD8186 Chemical Structure
AZD8186, CAS 1627494-13-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 61.00
10 mg In stock $ 101.00
25 mg In stock $ 177.00
50 mg In stock $ 320.00
100 mg In stock $ 531.00
500 mg In stock $ 1,180.00
1 mL * 10 mM (in DMSO) In stock $ 66.00
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Purity: 99.91%
Purity: 99.9%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AZD8186 is an effective and specific PI3Kβ/δ inhibitor (IC50: 4/12 nM).
Targets&IC50 PI3Kβ:4 nM, PI3Kδ:12 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]
Kinase Assay 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 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)
Molecular Weight 457.47
Formula C24H25F2N3O4
CAS No. 1627494-13-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3 mg/mL(6.6 mM)

DMSO: 84 mg/mL (183.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Barlaam B, et al. J Med Chem. 2015, 58(2), 943-962. 2. Hancox U, et al. Mol Cancer Ther. 2015, 14(1), 48-58. 3. Marques RB, et al. Eur Urol. 2015, 67(6), 1177-1185.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Obesity Compound Library Inhibitor Library Bioactive Compounds Library Max Anti-Ovarian Cancer Compound Library Anti-Prostate Cancer Compound Library Fluorochemical Library Angiogenesis related Compound Library

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Taurocholic acid VPS34 inhibitor 1 (Compound 19, PIK-III analogue) PI5P4Ks-IN-2 LX2343 Dehydroglyasperin D Uncarinic acid E 740 Y-P GNE-493

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Keywords

AZD8186 1627494-13-6 PI3K/Akt/mTOR signaling PI3K Phosphoinositide 3-kinase inhibit AZD 8186 Inhibitor AZD-8186 inhibitor

 

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