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AZD 6482

Catalog No. T6087 CAS 1173900-33-8

Synonyms: KIN 193, AZD6482

AZD 6482 (AZD6482) is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM.

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AZD 6482, CAS 1173900-33-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 262.00
50 mg	In stock	$ 490.00
100 mg	In stock	$ 715.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 99.95%

Purity: 99.91%

Purity: 99.79%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD 6482 (AZD6482) is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM.
Targets&IC50	PI3Kβ:10 nM, p110β:0.69 nM
In vitro	AZD6482 also inhibits PI3Kα, γ, and δ, with IC50 of 80 nM to 1.09 μM, which are significantly lower than its (+)-enantiomer (S-form). AZD6482 is an antiplatelet agent; it blocks platelet activation adhesion/aggregation and promotes platelet disaggregation in assay of washed platelet aggregation (WPA), with an IC50 value of 6 nM. Furthermore, by targeting PI3Kβ, AZD6482 specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, AZD6482 is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders. [1]
Kinase Assay	Assay of PI3K enzyme inhibition: The inhibition of PI3Kβ, PI3Kα, PI3Kγ, and PI3Kδ is evaluated in an AlphaScreen based enzyme activity assay using human recombinant enzymes. The assay measures PI3K-mediated conversion of PIP2 to PIP3. Biotinylated PIP3, a GST-tagged pleckstrin homology (PH) domain and the two AlphaScreen beads form a complex that elicits a signal upon laser excitation at 680 nm. The PIP3 formed in the enzyme reaction competes with the biotinylated PIP3 for binding to the PH domain thus reducing the signal with increasing enzyme product. The AZD6482 is dissolved in DMSO and added to 384 well plates. PBKβ, PBKα, PBKγ, or PBKδ is added in a Tris buffer (50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT, and 24 mM MgCl2) and allowed to preincubate with AZD6482 for 20 minutes prior to the addition of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 20 minutes by addition of stop solution containing EDTA and biotin-PIP3, followed by addition of detection solution containing GST-grpl PH and AlphaScreen beads. Plates are left for a minimum of 5 hours in the dark prior to analysis. The final concentration of DMSO, ATP and PIP2 in the assay are, 0.8%, 4 μM, and 40 μM, respectively. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration.
Cell Research	For assay of washed platelet aggregation (WPA), the platelet pellets are isolated from human blood and re-suspended to 2 × 1015/L in Tyrodes buffer (TB) containing 1 μM hirudin and 0.02 U/mL apyrase. Then, the platelet suspension is left to rest at room temperature for 30 min. Just prior to time for assay, CaCl2 is added to a final concentration of 2 mM. AZD6482, dissolved in DMSO, is added to a 96-well plate prior to the addition of the washed platelet suspension. The platelet suspension is preincubated with AZD6482 for 5 min. Light absorption at 650 nm is recorded before and after a 5 min plate shake and referred to as recording 0 (R0) and Rl. A mouse anti-human CD9 antibody is added (at a donor specific concentration) to each well prior to next 10 min plate shake and light absorption recording; R2. For data analysis, light absorbance in wells with TB are subtracted from all readings before percent aggregation is calculated according the formula: [(R1-R2)/R1] × 100 = % aggregation. Spontaneous aggregation or pro-aggregatory effect of the inhibitor is evaluated by the same formula, [(R0-Rl)/R0] × 100 = % aggregation. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration. (Only for Reference)

Synonyms	KIN 193, AZD6482
Molecular Weight	408.45
Formula	C22H24N4O4
CAS No.	1173900-33-8

Storage

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

Solubility Information

DMSO: 40.8 mg/mL (100 mM)

1eq. HCl: 4.1 mg/mL (10 mM)

References and Literature

1. Fjellstrom O, et al. US Patent, WO2009093972.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library PI3K-AKT-mTOR Compound Library Neuronal Differentiation Compound Library Oxidation-Reduction Compound Library HIF-1 Signaling Pathway Compound Library Angiogenesis related Compound Library

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CC-115 ETP-46464 SF2523 (R)-(-)-Rolipram STL127705 PIK-90 KU-57788 PI3K-IN-1

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AZD 6482 1173900-33-8 Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K Inhibitor AZD-6482 inhibit KIN-193 KIN193 KIN 193 AZD6482 Phosphoinositide 3-kinase inhibitor

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