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AZD-8835

Catalog No. T6774   CAS 1620576-64-8
Synonyms: AZD8835

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).

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AZD-8835 Chemical Structure
AZD-8835, CAS 1620576-64-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 105.00
25 mg In stock $ 198.00
50 mg In stock $ 289.00
100 mg In stock $ 497.00
1 mL * 10 mM (in DMSO) In stock $ 87.00
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Purity: 98.49%
Purity: 98.22%
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Biological Description
Chemical Properties
Storage & Solubility Information
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)
Synonyms AZD8835
Molecular Weight 469.54
Formula C22H31N9O3
CAS No. 1620576-64-8

Storage

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

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)

TargetMolReferences and Literature

1. Hudson K, et al. Mol Cancer Ther. 2016, 15(5):877-89. 2. Bernard Barlaam, et al. Bioorganic & Medicinal Chemistry Letters. 2015, 25(22):5155-5162.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Glycometabolism Compound Library Antioxidant Compound Library NO PAINS Compound Library Stem Cell Differentiation Compound Library

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Buparlisib SKI V GS-9901 MSC2360844 Dalbergioidin PI3Kδ-IN-12 GDC0084 Sennidin B

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Keywords

AZD-8835 1620576-64-8 PI3K/Akt/mTOR signaling PI3K inhibit AZD 8835 Inhibitor AZD8835 Phosphoinositide 3-kinase inhibitor

 

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